Your browser doesn't support javascript.
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 21
Filtrar
Mais filtros










Base de dados
Intervalo de ano de publicação
1.
Pest Manag Sci ; 75(12): 3273-3281, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31006964

RESUMO

BACKGROUND: N-Pyridylpyrazole derivatives have received continuous attention in agrochemical research during the last decade owing to their remarkable insecticidal or fungicidal potentials. To look for novel heterocyclic agrochemicals for increasing production of agriculture, a series of novel α-aminophosphonate derivatives containing N-pyridylpyrazole moiety were synthesized. RESULTS: The structures of the title compounds were confirmed via melting point, IR, 1 H NMR, 13 C NMR, 31 P NMR, HRMS and elemental analysis. The single crystal structure of diethyl (3-bromo-1-(3-chloropyridin-2-yl)-1H-pyrazol-5-yl)(2,6-dimethylphenylamino)methylphosphonate (compound 12b) was first reported. Moreover, the bioassays displayed that the title compounds exhibited modest or weak insecticidal activities against oriental armyworm at 200 µg mL-1 . The first investigation on the fungicidal potential of chlorantraniliprole showed no significant activities towards the six tested fungi found in this study, however, most of the title compounds displayed apparent in vitro fungicidal activity against some plant fungi, in particular excellent activities towards Physalospora piricola. Compounds 11a and 11b had EC50 values of 18.8 and 17.4 µg mL-1 , respectively, which were comparable with that of fungicide control triadimefon (EC50  = 24.7 µg mL-1 ) against Physalospora piricola. In addition, some compounds exhibited modest in vivo control efficacy at 0.5 mg mL-1 towards Sclerotinia sclerotiorum (11b: 30.1(±1.8)%), Rhizoctonia cerealis (11a: 20.4(±2.1)%; 11b: 30.2(±2.2)%), and Erysiphe graminis (11a: 30.3(±1.8)%; 12d: 40.2(±0.9)%). CONCLUSION: Compounds 11a, 11b and 12d could be promising new lead structures for the development and discovery of novel fungicides towards Physalospora piricola and Erysiphe graminis. The structure-activity relationship (SAR) analysis provided useful guidance and new understanding for the design of novel pyridylpyrazole-containing agrochemicals. © 2019 Society of Chemical Industry.


Assuntos
Ascomicetos/efeitos dos fármacos , Basidiomycota/efeitos dos fármacos , Fungicidas Industriais/farmacologia , Inseticidas/farmacologia , Mariposas/efeitos dos fármacos , Organofosfonatos/farmacologia , Animais , Fungicidas Industriais/síntese química , Inseticidas/síntese química , Larva/efeitos dos fármacos , Larva/crescimento & desenvolvimento , Mariposas/crescimento & desenvolvimento , Organofosfonatos/síntese química , Relação Estrutura-Atividade
2.
Eur J Med Chem ; 167: 472-484, 2019 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-30784880

RESUMO

Since pyrithiobac (PTB) is a successful commercial herbicide with very low toxicity against mammals, it is worth exploring its derivatives for an extensive study. Herein, a total of 35 novel compounds were chemically synthesized and single crystal of 6-6 was obtained to confirm the molecular structure of this family of compounds. The novel PTB derivatives were fully evaluated against various biological platforms. From the bioassay results, the best AHAS inhibitor 6-22 displayed weaker herbicidal activity but stronger anti-Candida activity than PTB did. For plant pathogenic fungi, 6-26 showed excellent activity at 50 mg/L dosage. Preliminary insecticidal activity and antiviral activity were also observed for some title compounds. Strikingly, 6-5 exhibited a promising inhibitory activity against SARS-CoV Mpro with IC50 of 4.471 µM and a low cellular cytotoxicity against mammalian 293 T cells. Based on the results of molecular modeling, HOMO-1 was considered to be a factor that affects AHAS inhibition and a possible binding mode of 6-5 with SARS-CoV Mpro was predicted. This is the first time that PTB derivatives have been studied as biological agents other than herbicides. The present research hence has suggested that more attentions should be paid to compounds belonging to this family to develop novel agrochemicals or medicines.


Assuntos
Benzoatos/síntese química , Benzoatos/farmacologia , Fungos/efeitos dos fármacos , Herbicidas/síntese química , Acetolactato Sintase/antagonistas & inibidores , Antivirais/síntese química , Antivirais/farmacologia , Benzoatos/química , Desenho de Fármacos , Herbicidas/farmacologia , Herbicidas/uso terapêutico , Modelos Moleculares , Estrutura Molecular , Vírus da SARS/efeitos dos fármacos
3.
Curr Med Res Opin ; 35(5): 887-891, 2019 05.
Artigo em Inglês | MEDLINE | ID: mdl-30366505

RESUMO

OBJECTIVE: The aim of this study was to determine the impact of adaptive iterative dose reduction 3 D (AIDR3D) on the improvement of shoulder image quality in low-radiographic dose head and neck CT angiography (CTA). MATERIALS AND METHODS: Ninety patients who underwent CTA examination were randomly divided into two groups, namely group A (n = 45) and B (n = 45). Patients in group A were scanned under 120 kV and 300 mA, with images reconstructed by filtered back projection (FBP), and patients in group B were scanned under 80 kV and auto mA with images reconstructed by AIDR3D. Image quality was accessed by two experienced radiologists. The noise, signal-to-noise ratio (SNR) and contrast-to-noise ratio (CNR) of common carotid artery (CCA) at C7 level, and radiation dosage were compared between the two groups. RESULTS: The score of CCA in group B was significantly higher than group A (p < 0.05), and there were no significant differences in the scores of carotid sinus and internal carotid artery between the two groups (p > 0.05). The score of intracranial artery in group B was lower than that of group A, however, the image quality in group B can meet the requirement of clinical diagnosis. The noise value of CCA at C7 level in group B was significantly lower than that of group A (p < 0.05). SNR and CNR values of CCA at C7 level in group B were significantly higher than those of group A (p < 0.05). Effective radiation dose in group B was significantly decreased compared with group A (p < 0.05). CONCLUSION: AIDR3D remarkably improved image quality in low-radiographic dose head and neck CTA over FBP, which made the low-dose CTA images meet the requirement of clinical diagnosis.

4.
J Invest Surg ; 32(8): 689-696, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-29693474

RESUMO

Objective: The objectives of this study were to examine the clinical profile of critically ill patients with septic acute kidney injury (AKI) and to investigate clinical characteristics associated with the outcome of patients. Methods: Data from 582 critically ill patients were collected and retrospectively reviewed. Patients were divided into two groups: without AKI development and with AKI development. Baseline characteristics, laboratory, and other clinical data were compared between these two groups, and correlations between the characteristics and AKI development were examined. Patients with AKI development were further divided into two groups according to the survival outcome, and variables associated with the outcome were determined. Results: AKI was developed in 54.12% (n = 315) of patients, and these patients had blood pressure, SOFA score, APACHE II score, GCS, and various blood chemistry and hematology characteristics significantly different from the patients without AKI. Demographic characteristics (e.g. age and weight) were comparable between the two groups of patients. Among the 315 patients with AKI, 136 of them died during the study period. Multivariate logistic regression analysis revealed that the outcome of patients was associated with lung infection, coagulation system dysfunction, staphylococcus aureus infection, and use of various treatments (epinephrine, norepinephrine, and the use of mechanical ventilation) after AKI development. Conclusion: AKI occurred in approximately half of the critically ill patients admitted to ICU. The site and type of infections, as well as the use of vasopressor agents, were associated with the outcome.

5.
Am J Chin Med ; 44(6): 1221-1236, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27744729

RESUMO

Drug-induced liver injury (DILI) is the most common cause of acute liver failure. Disruption of the Th17/Treg balance can lead to hepatic inflammation, which causes the main symptoms of DILI. Here we investigate the protective mechanisms of (-)-Epigallocatechin-3-gallate (EGCG) on triptolide (TP)-induced DILI that shows the Th17/Treg imbalance. Pretreatment with EGCG (5[Formula: see text]mg/kg) for 10 days before TP (0.5[Formula: see text]mg/kg) administration in mice significantly reduced the increased alanine aminotransferase (ALT) level ([Formula: see text]) induced by TP treatment. The hepatic histology analysis further proved that EGCG protected mice from TP-induced liver injury. The imbalance of Th17/Treg was induced by TP treatment, as shown by the upregulation of TLR4 and downregulation of Tim3 expression. EGCG pretreatment can maintain the expression of TLR4 and Tim3 at normal levels to restore the Th17/Treg imbalance. In addition, EGCG can block the TP-induced expression of the downstream targets of TLR4, including MyD88, NF[Formula: see text]B, and retinoid related orphan receptor (ROR-[Formula: see text]t), while EGCG can restore the TP inhibition of forkhead/winged-helix family transcriptional repressor p3 (FoxP3) that is the downstream target of Tim3. Consequently, EGCG pretreatment can effectively inhibit the Th17-related pro-inflammatory cytokine (e.g. IL-17 and IL-6) upregulation induced by TP treatment. However, TP inhibition of Treg-related anti-inflammatory cytokine IL-10 production was restored by EGCG pretreatment. Taken together, these results suggest that EGCG possesses significant protective properties against TP-induced hepatic inflammatory injury, and that these properties are carried out via the restoration of the Th17/Treg imbalance by the inhibition of the TLR4 signaling pathway and the enhanced activation of the Tim3 signaling pathway.


Assuntos
Catequina/análogos & derivados , Doença Hepática Induzida por Substâncias e Drogas/imunologia , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Diterpenos/efeitos adversos , Imunossupressores/efeitos adversos , Fenantrenos/efeitos adversos , Fitoterapia , Linfócitos T Reguladores/imunologia , Células Th17/imunologia , Animais , Catequina/administração & dosagem , Catequina/farmacologia , Doença Hepática Induzida por Substâncias e Drogas/etiologia , Citocinas/metabolismo , Modelos Animais de Doenças , Compostos de Epóxi/efeitos adversos , Feminino , Receptor Celular 2 do Vírus da Hepatite A , Mediadores da Inflamação/metabolismo , Camundongos , Camundongos Endogâmicos C57BL , Transdução de Sinais/efeitos dos fármacos , Receptor 4 Toll-Like , Regulação para Cima/efeitos dos fármacos
6.
Gastroenterol Res Pract ; 2016: 6242149, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27069474

RESUMO

Malignant peritoneal mesothelioma with invasion of the liver is an invariably fatal disease. We aimed to clarify the characteristics of malignant peritoneal mesothelioma cases with liver involvement. The clinical presentation, computed tomography images, and immunohistochemical and histopathological features of 5 patients with malignant peritoneal mesothelioma and liver involvement were evaluated. The diagnosis was established by imaging and immune profiles of the tumours. A review of 8 cases with primary or invading malignant mesothelioma in liver is presented. All 5 mesothelioma cases were asbestos-related. CT images of malignant peritoneal mesothelioma with the liver involvement typically showed that the lesion grew inside the liver along the capsule and was possibly accompanied by capsule breakthrough and extrahepatic infiltration. The tumours exhibited a common epithelioid appearance in all 5 patients and most cases revealed positive Cal, CK, and MC with negative CEA and HeP. Different from our findings, the review of literature revealed that most malignant mesothelioma of liver was due to primary intrahepatic malignant mesothelioma. Finally, we concluded that the diagnosis of malignant peritoneal mesothelioma cases with liver invasion is reliably achieved by the history of asbestos exposure, the characteristic CT imaging, and immune profiles of the tumours.

7.
Graefes Arch Clin Exp Ophthalmol ; 253(3): 389-98, 2015 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-25359392

RESUMO

BACKGROUND: Diabetic retinopathy is severe damage to the retina caused by complications of diabetes, and is the prevailing cause of blindness. Accumulating evidence from both animal models and humans suggests that the inflammatory process plays a key role in the development of diabetic retinopathy and is facilitated by innate immune response. The aim of this study was to examine whether the TLR4 signaling pathway was involved in the streptozotocin-induced diabetic rat retina. METHODS: Diabetes was induced by a single intraperitoneal injection of streptozotocin, and rat diabetic retinopathy was examined at 4 weeks of diabetes duration. Then the accumulated leukocytes were counted in vivo by acridine orange leukocyte fluorography, and the retinal vascular permeability was measured by the Evans blue assay. The expressions of TLR4 and its downstream signaling molecules were measured by RT-PCR or Western blot respectively. To evaluate the effect of blocking TLR4 on diabetic retinopathy, TAK-242, a selective TLR4 antagonist, was administered by intraperitoneal injection. RESULTS: Our results showed that the retina of diabetic rats demonstrated accumulated leukocytes and retinal vascular permeability. The mRNA and protein expressions of TLR4 were upregulated in streptozotocin-treated diabetic rat retina. Furthermore, the protein levels of TLR4 downstream signaling molecules were significantly increased in streptozotocin-treated animals. In addition, the protein levels of tumor necrosis factor (TNF)-α, interleukin (IL)-1ß, and interferon (IFN)-ß, three downstream proinflammatory cytokines of TLR4 signal transduction pathway, were also markedly increased in diabetic rats. Administration of TAK-242 attenuated leukocytes accumulated and retinal vascular permeability, and decreased TLR4 downstream signaling molecules and proinflammatory cytokines in streptozotocin-induced animals. CONCLUSIONS: Together, these data have demonstrated that TLR4 has a critical role in streptozotocin-induced diabetic retinopathy at the level of inflammatory cytokine induction, in both the MyD88-dependent and MyD88-independent pathways. TLR4 may become a new potential pharmacological target for treating diabetic retinopathy.


Assuntos
Diabetes Mellitus Experimental/metabolismo , Retinopatia Diabética/metabolismo , Retina/metabolismo , Transdução de Sinais/fisiologia , Receptor 4 Toll-Like/metabolismo , Animais , Glicemia/metabolismo , Barreira Hematorretiniana , Western Blotting , Permeabilidade Capilar , Ensaio de Imunoadsorção Enzimática , Injeções Intraperitoneais , Interferon beta/genética , Interferon beta/metabolismo , Interleucina-1beta/genética , Interleucina-1beta/metabolismo , Contagem de Leucócitos , Masculino , Ratos , Ratos Endogâmicos BN , Reação em Cadeia da Polimerase em Tempo Real , Sulfonamidas/farmacologia , Receptor 4 Toll-Like/antagonistas & inibidores , Receptor 4 Toll-Like/genética , Fator de Necrose Tumoral alfa/genética , Fator de Necrose Tumoral alfa/metabolismo
8.
Eur J Med Chem ; 86: 87-94, 2014 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-25147150

RESUMO

Succinate dehydrogenase inhibitors (SDHIs) are efficient fungicides that are widely used to control plant diseases caused by phytopathogenic fungi, although their effectiveness is undermined by the development of resistance across a range of different fungi. One of the most common structural features of SDHIs is their amide bond. The introduction of greater structural diversity to SDHIs is a promising strategy to delay the onset of resistance. A series of novel SDHIs containing a bioactive 1,2,3-triazole moiety have been designed and synthesized and their fungicidal and insecticidal activities evaluated. The results of these analyses show that most of the newly synthesized 1,2,3-trizole-4-carboxyl amide (ester) analogues exhibit good fungicidal activities, especially towards Sclerotinia sclerotiorum, and a structure-activity relationship study confirmed that the replacement of the amide group with an ester group had little effect on fungicidal activity, which could be provideous in terms of issues and metabolism. 1,6-Dimethyl phenyl was confirmed as the most efficient substituent of the current study when it was placed on both the amide and ester compounds. Interestingly, some of the newly synthesized compounds displayed good insecticidal activities against Culex pipiens pallens. The results of the current study show that these 1,2,3-triazole-4-carboxyl amide and ester analogues represent a new type of SDHI that could be used for the development of novel pesticides.


Assuntos
Antifúngicos/farmacologia , Ascomicetos/efeitos dos fármacos , Culex/efeitos dos fármacos , Desenho de Fármacos , Ésteres/farmacologia , Triazóis/farmacologia , Animais , Antifúngicos/síntese química , Antifúngicos/química , Relação Dose-Resposta a Droga , Ésteres/síntese química , Ésteres/química , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-Atividade , Triazóis/síntese química , Triazóis/química
9.
J Trauma Acute Care Surg ; 77(2): 351-5, 2014 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-25058264

RESUMO

BACKGROUND: Juxtahepatic vena cava (JHC) injury is difficult to handle because of JHC injury's specific position and liver obstruction. The traditional shunt method initially appeared to be useful but ultimately failed. Simple and effective methods are needed to solve it. METHODS: Firstly, the clinical data, including the computed tomography images, of 120 patients were collected. In addition, a JHC digital model was constructed based on computed tomography images. According to the digital model data, a circulation loop simulating the blood flow in the JHC was established. Secondly, we analyzed the hemodynamics of a JHC shunt with pig blood. Finally, the new shunt was designed based on the data obtained. The shunt consists of a covered stent and transfer device and was tested. RESULTS: The JHC has a three-dimensional cylindrical structure. The mean (SD) length of the retrohepatic vena cava is 78.21 (9.83) mm, which shows correlations with the patient's age and weight (r = -0.343 and 0.271, respectively, p < 0.05). An equation is obtained as follows: retrohepatic vena cava (millimeter) = 71.23 - 0.293 × age (year) + 0.32 × weight (kilogram). The shunt diameters must be 10 mm and 12 mm to maintain the blood pressure difference Point a and Point b at approximately 3.75 mm Hg (5 cm H2O), when the flow rate is 3,000 mL/min and 5,000 mL/min, respectively. The stent graft showed effective hemostasis in tests. However, it failed when the inferior vena cava was pulled harder. CONCLUSION: A temporary stent graft as a new shunt for JHC injury has not been previously reported. It is a combination of both a traditional operation and a simple endovascular technique, which showed effective hemostasis in tests.


Assuntos
Stents , Veia Cava Inferior/lesões , Derivação Arteriovenosa Cirúrgica/métodos , Prótese Vascular , Feminino , Veias Hepáticas/cirurgia , Humanos , Fígado/irrigação sanguínea , Masculino , Pessoa de Meia-Idade , Tomografia Computadorizada por Raios X , Enxerto Vascular/métodos , Veia Cava Inferior/diagnóstico por imagem , Veia Cava Inferior/cirurgia
10.
Org Biomol Chem ; 12(29): 5427-34, 2014 Aug 07.
Artigo em Inglês | MEDLINE | ID: mdl-24935054

RESUMO

Carboxylic acid amide (CAA) fungicides are an important class of agricultural fungicide with oomycete activity and low toxicity toward mammalian cells. To find CAA analogues with high activity against resistant pathogens, a series of substituted N-benzhydryl valinamide carbamate derivatives were designed and synthesized by introducing substituted aromatic rings into valinamide carbamate leads. Bioassays showed that some title compounds exhibited very good in vitro fungicidal activity against Phytophthora capsici and in vivo fungicidal activities against Pseudoperonospora cubensis. Topomer CoMFA was performed to explore the structure-activity relationship on the basis of the in vitro data. The dimethoxy substituted aromatic analogue 9e was found to display higher in vitro fungicidal activity against Phytophthora capsici than iprovalicarb but lower activity than mandipropamid, and higher in vivo fungicidal activity against Pseudoperonospora cubensis than dimethomorph at a dosage of 6.25 µg mL(-1).


Assuntos
Amidas/síntese química , Carbamatos/síntese química , Carbamatos/farmacologia , Ácidos Carboxílicos/síntese química , Ácidos Carboxílicos/farmacologia , Desenho de Fármacos , Fungicidas Industriais/síntese química , Amidas/química , Amidas/farmacologia , Carbamatos/química , Ácidos Carboxílicos/química , Fungos/efeitos dos fármacos , Fungicidas Industriais/química , Fungicidas Industriais/farmacologia , Testes de Sensibilidade Microbiana , Modelos Moleculares
11.
ACS Comb Sci ; 16(1): 17-23, 2014 Jan 13.
Artigo em Inglês | MEDLINE | ID: mdl-24147887

RESUMO

An ultrasound-promoted one-pot Passerini/hydrolysis reaction sequence has been developed for the synthesis of trifluoroatrolactamide derivatives using a diverse range of trifluoroacetophenones and isonitriles in acetic acid. Parallel synthesis in a centrifuge tube using a noncontact ultrasonic cell crusher was used in this study as an efficient method for the rapid generation of combinatorial trifluoroatrolactamide libraries, and subsequent biochemical evaluation of the resulting compounds indicated that they possessed excellent broad-spectrum fungicidal activities. N-(4-chlorophenyl)-2-(4-ethylphenyl)-3,3,3-trifluoro-2-hydroxypropanamide and N-(4-chlorophenyl)-3,3,3-trifluoro-2-hydroxy-2-(4-methoxyphenyl)propanamide, in particular, showed significant fungicidal activities against all of the fungal species tested in the current study.


Assuntos
Anilidas/farmacologia , Antifúngicos/farmacologia , Técnicas de Química Combinatória , Fungos/efeitos dos fármacos , Fenilpropionatos/farmacologia , Sonicação , Anilidas/síntese química , Anilidas/química , Antifúngicos/síntese química , Antifúngicos/química , Relação Dose-Resposta a Droga , Fungos/crescimento & desenvolvimento , Hidrólise , Testes de Sensibilidade Microbiana , Modelos Moleculares , Estrutura Molecular , Fenilpropionatos/síntese química , Fenilpropionatos/química , Relação Estrutura-Atividade
12.
Chem Cent J ; 7(1): 33, 2013 Feb 14.
Artigo em Inglês | MEDLINE | ID: mdl-23409923

RESUMO

BACKGROUND: Plant viruses cause many serious plant diseases and are currently suppressed with the simultaneous use of virucides and insecticides. The use of such materials, however, increases the amounts of pollutants in the environment. To reduce environmental contaminants, virucides with insecticidal activity is an attractive option. RESULTS: A series of substituted ferulic acid amide derivatives 7 and the corresponding hydrogenated ferulic acid amide derivatives 13 were synthesized and evaluated for their antiviral and insecticidal activities. The majority of the synthesized compounds exhibited good levels of antiviral activity against the tobacco mosaic virus (TMW), with compounds 7a, 7b and 7d in particular providing higher levels of protective and curative activities against TMV at 500 µg/mL than the control compound ribavirin. Furthermore, these compounds displayed good insecticidal activities against insects with piercing-sucking mouthparts, which can spread plant viruses between and within crops. CONCLUSIONS: Two series of ferulic acid derivatives have been synthesized efficiently. The bioassay showed title compounds not only inhibit the plant viral infection, but also prevented the spread of plant virus by insect vectors. These findings therefore demonstrate that the ferulic acid amides represent a new template for future antiviral studies.

13.
Comb Chem High Throughput Screen ; 16(6): 484-93, 2013 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-23360208

RESUMO

Heterogeneous copper-in-charcoal-catalyzed click synthesis in 96-well polypropylene filter plates is an efficient method for the rapid generation of sufficient pure 2-alkoxyl-2-(1,2,3-triazole-1-yl) acetamide derivatives library by simple filtration, which directly assay the products for larvicidal activity against mosquitoes. In this procedure, copper nanoparticles on charcoal were arrayed into each well on a 96-well plate, reagents were delivered using a pipette gun, and a constant temperature shaker bath was used to complete the click reaction in 24-72 hours under temperature-controlled conditions. The results of bioassays indicated that the target compounds possessed excellent larvacidal activities against mosquitoes. In particular, the larvacidal activities against mosquitoes of compounds 8[2,3] and 8[7,1] at 2 µg.mL⁻¹ were 100% and 73% respectively.


Assuntos
Acetamidas/farmacologia , Química Click , Culicidae/efeitos dos fármacos , Culicidae/crescimento & desenvolvimento , Inseticidas/síntese química , Inseticidas/farmacologia , Bibliotecas de Moléculas Pequenas/síntese química , Bibliotecas de Moléculas Pequenas/farmacologia , Triazóis/farmacologia , Acetamidas/síntese química , Animais , Catálise , Carvão Vegetal/química , Cobre/química , Inseticidas/química , Larva/efeitos dos fármacos , Estrutura Molecular , Bibliotecas de Moléculas Pequenas/química , Triazóis/síntese química
14.
Chem Cent J ; 6(1): 99, 2012 Sep 11.
Artigo em Inglês | MEDLINE | ID: mdl-22963735

RESUMO

BACKGROUND: Culex is an important mosquito as vectors for the transmission of serious diseases, such as filariasis, West Nile virus, dengue, yellow fever, chikungunya and other encephalitides. Nearly one billion people in the developing countries are at risk. In order to discover new bioactive molecules and pesticides acting on mosquito, we designed active amide structure and synthesized a series of novel diamide derivatives. RESULTS: A series of novel diamide derivatives were designed and synthesized. Their structures were characterized by 1 H NMR, FTIR and HRMS. The single crystal structure of compound 6n was determined to further elucidate the structure. Biological activities of these compounds were tested. Most of them exhibited higher mosquito larvicidal activity. Especially compound 6r displayed relatively good activity to reach 70% at 2 µg/mL. CONCLUSION: A practical synthetic route to amide derivatives by the reaction of amide with another acid is presented. This study suggests that the diamide derivatives exhibited good effective against mosquito.

15.
Zhonghua Yi Xue Za Zhi ; 92(37): 2652-5, 2012 Oct 09.
Artigo em Chinês | MEDLINE | ID: mdl-23290071

RESUMO

OBJECTIVE: To evaluate the effects of heart rate (HR) on image quality and radiation dose of "triple rule-out" 320-row-640-slice multidetector computed tomography (MDCT) scan in patients with acute chest pain. METHODS: Retrospective analyses were performed for the clinical and imaging data of 38 cases with acute chest pain. All patients received 320-row-640-slice MDCT. Scanning program was electrocardiography-gated helical scan of full chest (160×0.5 mm). Based upon different heart rates, they were divided into A and B groups (A: n = 18, HR ≤ 65 bpm; B: n = 20, HR > 65 bpm). T he results of image quality and radiation dose of pulmonary artery, aorta and coronary artery between A and B group were evaluated respectively. T he subjective quality indicators of coronary artery were excellent, good, qualified and poor. RESULTS: (1) Overall quality assessment: the mean CT values of ascending aortic root, main pulmonary artery, right coronary artery and left coronary artery were (412 ± 79) HU, (381 ± 107) HU, (408 ± 79) HU, (406 ± 79) HU respectively; the contrast-noise ratio (CNR) of ascending aorta root was 12 ± 7; excellent stage of subjective quality assessment of coronary artery accounted for 66.13%, good and qualified stage 32.79% and poor stage 1.08%. T he mean radiation dose was 22 ± 3 mSv. (2) The mean CT value between A and B groups of ascending aortic root, main pulmonary artery, right coronary artery and left coronary artery, and CNR of ascending aortic root [(421 ± 62) HU vs (404 ± 93) HU, (402 ± 103) HU vs (362 ± 110) HU, (417 ± 62) HU vs (400 ± 92) HU, (417 ± 63) HU vs (397 ± 92) HU, 10 ± 3 vs 13 ± 8 respectively] were not statistically different (P > 0.05); the number of segments of excellent subjective quality assessment and evaluable (excellent, good and qualified) of coronary artery between A and B groups were statistically significant (P = 0.001, P = 0.019). Group A was better than Group B. But the number of diagnosed segments of Group B still accounted for 97.9%. T he radiation doses of two groups were 18 ± 6 and 26 ± 5 mSv respectively. Group B was significantly higher than Group A and significant difference existed between two values (P = 0.000). CONCLUSION: The "triple rule-out" 320-row-640-slice MDCT scan may acquire high quality images of aorta, pulmonary arteries and coronary arteries for both high and low HR groups. With a low contrast-medium dosage and patient radiation dose, it is ideal for an etiological diagnosis of acute chest pain. Reducing HR further improves image quality and lowers radiation dose.


Assuntos
Dor no Peito/diagnóstico por imagem , Frequência Cardíaca , Tomografia Computadorizada Multidetectores , Tomografia Computadorizada por Raios X/métodos , Adulto , Idoso , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Doses de Radiação , Estudos Retrospectivos
16.
Chem Biol Drug Des ; 78(4): 695-9, 2011 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-21736703

RESUMO

In an attempt to search for potent antifungal agents, a series of novel 1-substituted phenyl-4-[N-[(2'-morpholinothoxy)phenyl]aminomethyl]-1H-1,2,3-triazoles 5a-m was designed and synthesized via Huisgen cycloaddition reaction between various (2-morpholinoethoxy)-N-(prop-2-ynyl)aniline and different azidobenzene. Their chemical structures were characterized by (1) H NMR and elemental analysis. A cleaner reaction with milder conditions and satisfactory yields was observed in the micorwave-assisted synthesis of 4a-c. The fungicidal activity of some target compounds were evaluated in vitro against Fusarium omysporum, Physalospora piricola, Alternaria solani, Cercospora arachidicola and Gibberella zeae at 50 µg/mL. The bioassay results indicated that some compounds exhibited moderate fungicidal activities. Furthermore, compound 5h displayed equal activity to the positive control compounds against Alternaria solani.


Assuntos
Antifúngicos/química , Antifúngicos/farmacologia , Fungos/efeitos dos fármacos , Triazóis/química , Triazóis/farmacologia , Antifúngicos/síntese química , Desenho de Fármacos , Humanos , Micoses/tratamento farmacológico , Relação Estrutura-Atividade , Triazóis/síntese química
17.
World J Gastroenterol ; 17(15): 2028-36, 2011 Apr 21.
Artigo em Inglês | MEDLINE | ID: mdl-21528083

RESUMO

AIM: To investigate the expression of markers that are correlated with the prognosis of colorectal cancer (CRC) patients. METHODS: One hundred and fifty-six CRC patients were followed up for more than 3 years after radical surgery. Immunohistochemical (IHC) analysis was performed to detect the expression of 14 pathway-related markers (p53, APC, p21ras, E-cadherin, endothelin-B receptor, Shp2, ADCY-2, SPARCL1, neuroligin1, hsp27, mmp-9, MAPK, MSH2 and rho) in specimens from these patients. Bioinformatics analysis involving a Support Vector Machine (SVM) was used to determine the best prognostic model from combinations of these markers. RESULTS: Seven markers (SPARCL1, Shp2, MSH2, E-cadherin, p53, ADCY-2 and MAPK) were significantly related to the prognosis and clinical pathological features of the CRC patients (P < 0.05). Prognostic models were established through SVM from combinations of these 7 markers and proved able to differentiate patients with dissimilar survival, especially in stage II/III patients. According to the best prognostic model, the p53/SPARCL1 model, patients having high p53 and low SPARCL1 expression had about 50% lower 3-year survival than others (P < 0.001). CONCLUSION: SPARCL1, Shp2, MSH2, E-cadherin, p53, ADCY-2 and MAPK are potential prognostic markers in CRC. A p53/SPARCL1 bioinformatics model may be used as a supplement to tumor-nodes-metastasis staging.


Assuntos
Adenilil Ciclases/metabolismo , Caderinas/metabolismo , Proteínas de Ligação ao Cálcio/metabolismo , Neoplasias Colorretais/metabolismo , Proteínas da Matriz Extracelular/metabolismo , Proteínas Quinases Ativadas por Mitógeno/metabolismo , Proteína 2 Homóloga a MutS/metabolismo , Proteína Tirosina Fosfatase não Receptora Tipo 11/metabolismo , Proteína Supressora de Tumor p53/metabolismo , Biomarcadores Tumorais/metabolismo , Neoplasias Colorretais/diagnóstico , Neoplasias Colorretais/patologia , Humanos , Estimativa de Kaplan-Meier , Estadiamento de Neoplasias , Prognóstico
18.
Eur J Med Chem ; 46(5): 1463-72, 2011 May.
Artigo em Inglês | MEDLINE | ID: mdl-21356570

RESUMO

A series of novel analogs of pyrrole alkaloid were designed and synthesized by a facile method and their structures were characterized by 1H NMR, 13C NMR and high-resolution mass spectrometry (HRMS). The structure of compound 2a was identified by 2D NMR including heteronuclear multiple-quantum coherence (HMQC), heteronuclear multiple-bond correlation (HMBC) and H-H correlation spectrometry (H-H COSY) spectra. Their antifungal activities against five fungi were evaluated, and the results indicated that some of the title compounds showed moderate fungicidal activities in vitro against Alternaria solani, Cercospora arachidicola, Fusarium omysporum, Gibberella zeae and Physalospora piricola at the dosage of 50 µg mL(-1). Compound 2a and 3a exhibited good activities against P. piricola at low dosage.


Assuntos
Alcaloides/farmacologia , Antifúngicos/farmacologia , Desenho de Fármacos , Fungos/efeitos dos fármacos , Pirróis/farmacologia , Alcaloides/síntese química , Alcaloides/química , Antifúngicos/síntese química , Antifúngicos/química , Testes de Sensibilidade Microbiana , Estrutura Molecular , Pirróis/síntese química , Pirróis/química , Estereoisomerismo , Relação Estrutura-Atividade
19.
J Agric Food Chem ; 58(6): 3651-60, 2010 Mar 24.
Artigo em Inglês | MEDLINE | ID: mdl-20166721

RESUMO

A series of novel 6-aminophenazine-1-, 7-aminophenazine-1- and 8-aminophenazine-1-carboxylate derivatives were synthesized by a facile method, and their structures were characterized by (1)H NMR, (13)C NMR and high-resolution mass spectrometry. Some unexpected byproducts V-7b-V-8d were noticed and isolated, and their structures were identified by 2D NMR spectra including heteronuclear multiple-quantum coherence (HMQC), heteronuclear multiple-bond correlation (Hmbc) and H-H correlation spectrometry (H-H COSY) approach. Their fungicidal activities against five fungi were evaluated, which indicated that most of the title compounds showed low fungicidal activities in vitro against Alternaria solani, Cercospora arachidicola, Fusarium omysporum, Gibberella zeae, and Physalospora piricola at a dosage of 50 microg mL(-1), while compounds IV-6a and IV-6b exhibited excellent activities against P. piricola at that dosage. Compound IV-6a could be considered as a leading structure for further design of fungicides.


Assuntos
Fungos/efeitos dos fármacos , Fungicidas Industriais/síntese química , Fungicidas Industriais/farmacologia , Fungicidas Industriais/química , Estrutura Molecular
20.
Chin J Integr Med ; 15(4): 284-8, 2009 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-19688317

RESUMO

OBJECTIVE: To investigate the inhibitory effects of Kangjia Pill (KJP) on the cell proliferation in rat goiter model induced by methimazole (MMI). METHODS: Fifty-six Wistar rats were randomly divided into four groups: the normal group, MMI model group (MMI), low dose of KJP group (LKJP), and high dose of KJP (HKJP). Except the normal group (20 rats), the other groups (12 rats in each) were given 0.04% (w/v) MMI through the drinking water until the end of the experiment. One week later, the rats in the LKJP and HKJP groups were given KJP by gastrogavage at the dose of 250 mg/(kg x d) and 1,000 mg/(kg x d), respectively for 12 weeks. The relative thyroid weight (mg/100 g body weight) of each rat was accessed. The expression of proliferating cell nuclear antigen (PCNA) was determined by immunohistochemistry, and the correlation analysis between the PCNA positive thyrocytes and the relative thyroid weight was performed. The expressions of PCNA and cyclin D1 were examined with Western blotting. RESULTS: After KJP treatment for 12 weeks, compared with the MMI group, the relative thyroid weight of the HKJP group decreased significantly, and the positive thyrocyte populations of PCNA in the two KJP groups reduced markedly (all P<0.05). The correlation analysis showed that PCNA was closely correlated with thyrocyte proliferation (r=0.685, P<0.05). KJP significantly decreased the protein expression of PCNA and cyclin D1 in the thyroid specimens (P<0.05), the high dose showed better effects. CONCLUSION: KJP played a therapeutic role via inhibiting cell proliferation in the rat goitrous glands.


Assuntos
Proliferação de Células/efeitos dos fármacos , Medicamentos de Ervas Chinesas/administração & dosagem , Bócio/tratamento farmacológico , Glândula Tireoide/efeitos dos fármacos , Glândula Tireoide/patologia , Animais , Ciclina D1/metabolismo , Modelos Animais de Doenças , Regulação para Baixo/efeitos dos fármacos , Avaliação Pré-Clínica de Medicamentos , Medicamentos de Ervas Chinesas/farmacologia , Bócio/induzido quimicamente , Bócio/metabolismo , Bócio/patologia , Masculino , Metimazol , Tamanho do Órgão/efeitos dos fármacos , Antígeno Nuclear de Célula em Proliferação/metabolismo , Distribuição Aleatória , Ratos , Ratos Wistar , Comprimidos , Glândula Tireoide/metabolismo
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA