RESUMO
Three series of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety (5a-k, 6a-i, and 7a-i) have been synthesized, characterized and evaluated for their antibacterial activity. Some of these displayed potent antibacterial activity against several Gram-positive and Gram-negative bacterial strains (including multidrug-resistant clinical isolates) with minimum inhibitory concentration (MIC) values in the range of 4-64 µg/mL and minimum bactericidal concentration (MBC) values in the range of 8-256 µg/mL. Compared with previously reported rhodanine derivatives, these compounds exhibited a broad spectrum of antibacterial activity by means of introducing 4-amino-5-aryl-1,2,4-triazole-3-thione moiety. Notably, compound 5f exhibited good antibacterial activity against Staphylococcus aureus RN 4220, S. aureus 209, S. aureus 503, Gram-negative bacteria (Escherichia coli 1924), and Candida albicans 7535 with MBC values of 8 or 16 µg/ml. All of the compounds synthesized in the current Letter were characterized by (1)H NMR, (13)C NMR, infrared and mass spectroscopy.
Assuntos
Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Rodanina/análogos & derivados , Rodanina/farmacologia , Triazóis/química , Triazóis/farmacologia , Anti-Infecciosos/síntese química , Candida albicans/efeitos dos fármacos , Candidíase/tratamento farmacológico , Escherichia coli/efeitos dos fármacos , Infecções por Escherichia coli/tratamento farmacológico , Humanos , Rodanina/síntese química , Infecções Estafilocócicas/tratamento farmacológico , Staphylococcus aureus/efeitos dos fármacos , Tionas/síntese química , Tionas/química , Tionas/farmacologia , Triazóis/síntese químicaRESUMO
Three series of 1,3-diaryl pyrazole derivatives bearing aminoguanidine or furan-2-carbohydrazide moieties have been synthesized, characterized and evaluated for antibacterial and anti-inflammatory activities. Most of the synthesized compounds showed potent inhibition of several Gram-positive bacterial strains (including multidrug-resistant clinical isolates) and Gram-negative bacterial strains with minimum inhibitory concentration values in the range of 1-64 µg/mL. Compounds 6g, 6l and 7l presented the most potent inhibitory activity against Gram-positive bacteria (e.g. Staphylococcus aureus 4220), Gram-negative bacteria (e.g. Escherichia coli 1924) and the fungus, Candida albicans 7535, with minimum inhibitory concentration values of 1 or 2 µg/mL. Compared with previous studies, these compounds exhibited a broad spectrum of inhibitory activity. Furthermore, compound 7l showed the greatest anti-inflammatory activity (93.59% inhibition, 30 min after intraperitoneal administration), which was more potent than the reference drugs ibuprofen and indomethacin.
Assuntos
Antibacterianos/farmacologia , Anti-Inflamatórios não Esteroides/farmacologia , Furanos/farmacologia , Pirazóis/farmacologia , Animais , Antibacterianos/síntese química , Anti-Inflamatórios não Esteroides/síntese química , Antifúngicos/síntese química , Antifúngicos/farmacologia , Candida albicans/efeitos dos fármacos , Farmacorresistência Bacteriana Múltipla , Furanos/síntese química , Furanos/química , Bactérias Gram-Negativas/efeitos dos fármacos , Cocos Gram-Positivos/efeitos dos fármacos , Ibuprofeno/farmacologia , Indometacina/farmacologia , Camundongos , Pirazóis/síntese químicaRESUMO
Four series of [1,2,4]triazolo[3,4-a]phthalazine and tetrazolo[5,1-a]phthalazine derivatives bearing substituted piperazine moieties were synthesized and evaluated for their positive inotropic activity by measuring the left atrium stroke volume in isolated rabbit-heart preparations. Several compounds were developed and showed favorable activities compared to the standard drug milrinone, with (4-([1,2,4]triazolo[3,4-a]phthalazin-6-yl)piperazin-1-yl)(p-tolyl)methanone (5g) being identified as the most potent with an increased stroke volume of 19.15±0.22% (milrinone: 2.46±0.07%) at a concentration of 3×10(-5) M. A preliminary study of mechanism of action revealed that 5g displayed its positive inotropic effect may be related to the PDE-cAMP-PKA signaling pathway. Compounds exhibiting inotropic effects were also evaluated in terms of the chronotropic effects.
Assuntos
Ftalazinas/farmacologia , Piperazinas/química , Volume Sistólico/efeitos dos fármacos , Triazóis/farmacologia , Função Ventricular Esquerda/efeitos dos fármacos , Animais , Relação Dose-Resposta a Droga , Ftalazinas/síntese química , Ftalazinas/química , Piperazina , Coelhos , Relação Estrutura-Atividade , Triazóis/síntese química , Triazóis/químicaRESUMO
OBJECTIVES: To study the relationship between serum levels of some inflammatory markers and stability of carotid plaques in the patients with carotid plaques and evaluate the ability of each serum marker in identifying vulnerable carotid plaques. METHODS: The study included 65 consecutive patients with carotid plaques confirmed by imaging examinations from March 2008 to March 2010. All the patients were classified as stable plaques group (n = 21) and unstable plaques group (n = 44) according to the characteristic findings of the plaques in MRI such as the thickness of fibrous cap, the existence of large lipid core and the intra-plaque hemorrhage. The patients of unstable plaques group were further classified as unruptured plaques group (n = 29) and rupture plaques group (n = 15) according to the integrity of fibrous cap. Serum levels of soluble cluster of differentiation 40 ligand (sCD40L), matrix metalloproteinase 9 (MMP-9) and pregnancy-associated plasma protein A (PAPP-A) were determined by ELISA. RESULTS: Serum levels of sCD40L and MMP-9 in patients of unstable plaques group, unruptured plaques group and rupture plaques group were all significantly enhanced compared to individuals of stable plaques group (SCD40L: χ(2) = 6.45, 12.04 and 16.23, P < 0.01; MMP-9; F = 2.55, 5.10 and 4.69, P < 0.05). Serum levels of PAPP-A in patients of unstable plaques group and rupture plaques group were all significantly enhanced compared to individuals of stable plaques group (χ(2) = 11.71 and 13.55, P < 0.05). Serum levels of PAPP-A in patients of rupture plaques group were significantly enhanced compared to individuals of unruptured plaques group (χ(2) = 13.19, P = 0.000). sCD40L ≥ 673.22 ng/L (OR = 22.47, 95%CI: 2.11 - 239.81, P = 0.010), MMP-9 ≥ 84.09 µg/L (OR = 10.01, 95%CI: 1.74 - 57.78, P = 0.010) and PAPP-A ≥ 0.101 µg/L (OR = 14.29, 95%CI: 2.69 - 75.90, P = 0.002) were all significantly correlated with the vulnerability of carotid plaques. CONCLUSIONS: There appear to be a relationship between the serum levels of sCD40L, MMP-9 and PAPP-A and the stability of carotid plaques in patients with carotid plaques. High serum levels of the above-mentioned markers may indicate that the plaques were vulnerable or ruptured.
Assuntos
Ligante de CD40/sangue , Estenose das Carótidas/sangue , Metaloproteinase 9 da Matriz/sangue , Proteína Plasmática A Associada à Gravidez/metabolismo , Idoso , Idoso de 80 Anos ou mais , Feminino , Humanos , Masculino , Pessoa de Meia-IdadeRESUMO
OBJECTIVE: To study the necessity, feasibility, security of carotid angioplasty and stenting (CAS) for symptomatic carotid stenosis combined with kinking. METHODS: Twelve patients with symptomatic carotid stenosis and kinking demonstrated by digital subtraction angiography (DSA) received CAS from December 2003 to December 2009. There were 9 male and 3 female patients, age ranged from 59 to 77 years (mean 69.3 years). All the patients' clinical, imaging, intervention and follow up data were collected and analyzed. RESULTS: All CAS procedures were successfully performed with 14 self-expandable stents placed. The mean degree of stenosis was reduced from 85.6% before stenting to 11.2% after stenting, the angle of kinking, according to Metz' category, were improved from less than 90° to more than 120° in each case. No perioperative procedure related stroke and transient ischemic attack (TIA) occurred. The clinical symptoms and signs of cerebral ischemia were improved or disappeared for all patients. During follow-up of these 12 patients for 6 to 72 months, one patient experienced ipsilateral carotid territory TIA and another patient experienced contralateral carotid territory TIA. DSA follow up of 5 patients demonstrated 1 case with in-stent restenosis and arterial kinking remote to the stent of internal carotid artery. CAS were performed again and CT angiography follow up demonstrated no kinking and restenosis 2 years after the intervention. Duplex scan of the other 7 patients demonstrated neither kinking nor restenosis. CONCLUSIONS: CAS seems to be feasible and safe for the patients with symptomatic kinking and stenosis, and maybe helpful to lower the risk of cerebral ischemia, but further study is needed.
Assuntos
Angioplastia com Balão/métodos , Estenose das Carótidas/cirurgia , Idoso , Estudos de Viabilidade , Feminino , Seguimentos , Humanos , Masculino , Pessoa de Meia-Idade , Stents , Resultado do TratamentoRESUMO
Subdural contrast effusion secondary to endovascular treatment is exceptionally rare and might be mistaken as subdural hematoma because of similar hyperattenuation on computer tomography. The authors present the case of a 13-month-old girl with a history of increased head circumference and developmental retardation. Cerebral digital subtraction angiography showed a high-flow pial arteriovenous fistula fed by multiple arteries on the right cerebellar surface, with occlusion of the right sigmoid sinus and severe stenosis of the left sigmoid sinus. Staged endovascular treatments were performed to eliminate the fistula. Follow-up head computer tomography scans performed 3 h after both procedures demonstrated typical high-density subdural effusion with computer tomography attenuation value similar to hemorrhage. These effusions did not aggravate the condition and disappeared spontaneously 32 h after the first treatment and 29 h after the second, respectively.
Assuntos
Fístula Arteriovenosa , Embolização Terapêutica , Procedimentos Endovasculares , Derrame Subdural , Fístula Arteriovenosa/diagnóstico por imagem , Fístula Arteriovenosa/etiologia , Fístula Arteriovenosa/terapia , Angiografia Cerebral , Criança , Procedimentos Endovasculares/efeitos adversos , Feminino , Humanos , LactenteRESUMO
OBJECTIVE: To evaluate the feasibility and safety of endovascular treatment of ruptured and unruptured intracranial very small aneurysms (< or = 3 mm in maximal diameter). METHODS: Forty-eight intracranial very small aneurysms in 44 patients treated with endovascular therapy from June 2001 to August 2009 were reviewed retrospectively in clinical, imaging, interventional and follow-up data. Among 44 patients, there were 20 males and 24 females with a mean age of 57.8 years old. The Hunt-Kosnik grade was as follows: Grade 0 (n = 11); Grades I & II (n = 23); Grades III & IV (n = 9); and ungraded (n = 1). The sizes of 48 aneurysms were not more than 3 mm in maximal diameter. The locations of aneurysms were as follows: ACoA (n = 11), MCA (n = 8), PCoA (n = 14), ICA (n = 12), pericallosal artery (n = 1), VA (n = 1) and PICA (n = 1). Thirty-nine aneurysms were embolized with coil, of which 13 with stent assistance and 6 by balloon remodeling technique. The other 9 aneurysms underwent sole stent placement in parent artery. RESULTS: Among 39 coiling aneurysms, 100% occlusion was achieved in 9 aneurysms, 90% in 20, 80% in 9 and less than 80% in 1 respectively. Only one aneurysm ruptured during coiling. Two patients had transient hemiparesis and one patient had ataxia caused by bilateral cerebellar infarction postoperatively. All patients were clinically followed up for 4-90 months and no recurrent hemorrhage occurred. Thirteen patients received repeat angiography at 4-72 months post-treatment. And no radiological re-growth was detected. CONCLUSION: Endovascular treatment of ruptured and unruptured intracranial very small aneurysms seems to be technically feasible, relatively safe and practically effective.
Assuntos
Arteríolas/lesões , Embolização Terapêutica/métodos , Aneurisma Intracraniano/terapia , Adulto , Idoso , Idoso de 80 Anos ou mais , Feminino , Humanos , Aneurisma Intracraniano/patologia , Masculino , Pessoa de Meia-Idade , Estudos Retrospectivos , Ruptura , Resultado do TratamentoRESUMO
OBJECTIVES: To investigate adverse factors that may hinder successful placement and stabilization of the microcatheter during endovascular therapy of micro-intracranial aneurysms (≤ 3 mm in maximum diameter), and to explore the relevant managements. METHODS: Forty-six patients with fifty-one micro-intracranial aneurysms treated by endovascular therapy from June 2001 to October 2009 were retrospectively analyzed for their intervention data. RESULTS: Adverse factors of optimal micro-catheterization mainly included, tortuosity of the proximal vessels (PVs) and the parent artery (PA), relative large gap in diameter among the PVs, the PA and the microcatheter, relative large divergence in direction among the PVs, the PA and the aneurysm dome, and stent deployed in the PA. CONCLUSIONS: Carefully considering the direction of the PVs and the PA, the aneurysm's location and dome orientation, choosing the microcatheter and microwire after balancing among their physical properties, as well as utilizing balloon and/or stent assistance, can facilitate micro-catheterization during endovascular treatment of micro-intracranial aneurysms.
Assuntos
Cateterismo/métodos , Embolização Terapêutica/métodos , Aneurisma Intracraniano/terapia , Adulto , Idoso , Idoso de 80 Anos ou mais , Feminino , Seguimentos , Humanos , Masculino , Pessoa de Meia-Idade , Estudos Retrospectivos , Stents , Resultado do TratamentoRESUMO
OBJECTIVE: To investigate the effect of two clopidogrel pretreatment duration on platelet activation in patients undergoing stenting. METHODS: From July 2006 to December 2007 40 elective carotid or vertebral artery stenting patients were assigned into two groups: Group A (n = 24) initiated clopidogrel (75 mg/d) > or = 5 d before stenting; group B (n = 16) initiated 3 - 4 days. Platelet-monocyte aggregates and fibrinogen receptors analyzed by flow cytometric, and platelet aggregation tests using optical aggregometry, as well as serum soluble CD40 ligand quantified by enzyme-linked immunosorbent assay were assessed in peripheral blood samples obtained immediately before and at 0.5, 18 h and 6 d after stenting. RESULTS: Platelet-monocyte aggregates, fibrinogen receptors and serum soluble CD40 ligand were higher in group B than in group A (14.59% vs 8.70%, P = 0.012; 4.87% vs 2.42%, P = 0.024; 5.79 microg/L vs 2.64 microg/L, P = 0.020) at 18 h after stenting. Serum soluble CD40 ligand was higher in group B than in group A (0.49 microg/L vs 0.31 microg/L, P = 0.033) at 0.5 h after stenting. CONCLUSIONS: Premedication before stenting with clopidogrel 75 mg/d merely 3 - 4 d may be insufficient to achieve adequate platelet inhibition, whereas clopidogrel initiated at least 5 d could obtain preferable clinical antiplatelet efficacy.
Assuntos
Ativação Plaquetária/efeitos dos fármacos , Inibidores da Agregação Plaquetária/administração & dosagem , Stents , Ticlopidina/análogos & derivados , Adulto , Idoso , Idoso de 80 Anos ou mais , Estenose das Carótidas/sangue , Estenose das Carótidas/terapia , Clopidogrel , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Ticlopidina/administração & dosagem , Fatores de TempoRESUMO
OBJECTIVE: To observe the changes of nitric oxide (NO) and endothelin (ET) serum level in the Guangxi BA-MA minipigs whose carotid arteries were injured by balloon denudation and in the patients with carotid stent assisted angioplasty. METHODS: Twelve Guangxi BA-MA minipigs were chosen. High fat/cholesterol feeding and endovascular balloon denudation were used to create a carotid artery atherosclerotic stenosis animal model. Blood samples were collected from peripheral veins before starting the procedure, and again, at 2 and 3 weeks after the procedure, respectively. Serum NO and ET concentrations of blood samples were tested. Nineteen patients with carotid artery stenosis who underwent stent assisted angioplasty were randomly selected, and their serum NO and ET were tested using the same methods as above. RESULTS: In the animal group, there was a significant decrease of mean NO concentration at 2 weeks after carotid injury (t-test, P < 0.05), however, no significant change of ET was observed. A very significant increase of ET was observed at 3 weeks after the procedure (t-test, P < 0.01). In the patient group, there were no significant differences among serum NO or ET concentration of peripheral vein blood before, immediately after, and 6 h after the endovascular treatment. CONCLUSIONS: In this study, a decrease of NO concentration and an increase of ET concentration of peripheral vein blood are found in BA-MA minipigs after carotid arteries are injured by balloon denudation, which might be a cue for the formation of atherosclerosis. However, no significant changes are observed in this group of patients who underwent carotid angioplasty treatment. Therefore, further studies are needed.
Assuntos
Angioplastia com Balão , Estenose das Carótidas/sangue , Endotelinas/sangue , Óxido Nítrico/sangue , Stents , Idoso , Animais , Artérias Carótidas/cirurgia , Estenose das Carótidas/cirurgia , Modelos Animais de Doenças , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Período Pós-Operatório , Distribuição Aleatória , Suínos , Porco MiniaturaRESUMO
OBJECTIVES: To explore influencing factors of regional cerebral blood flow (rCBF) in geriatric carotid stenosis, and to analyze changes of rCBF and clinical symptoms after carotid stenting. METHODS: During August 2005 and April 2008, 68 geriatric patients of carotid stenosis having SPECT examination in our hospital were retrospectively studied, whose diagnosis was approved by angiography. Correlated rCBF was compared separately in different stenotic degrees of carotid stenosis, in unilateral or bilateral stenosis, accompanied with vertebrobasilar stenosis (VBS) or not, with collateral circulation or not, before and after carotid stenting. RESULTS: When patients of unilateral carotid stenosis were grouped by different clinical factors, cases of patients with reduced rCBF were compared using chi(2) test: the P value was 0.046 and 0.020 when comparing group of stenotic degree 90% - 99% with group 70% - 89% and group 50% - 69%; the P value was 0.927 between group accompanied with VBS and group without; the P value was 0.222 between group with collateral circulation and group without. When comparing reduced rCBF cases between unilateral and bilateral carotid stenosis, the P value was 0.046. After carotid stenting, 76% of patients had their rCBF improved, and also the scores of presenting symptoms evaluated by modified Rankin scale were elevated from 1.4 +/- 0.7 on admission to 0.4 +/- 0.3 postoperatively (P < 0.001). CONCLUSIONS: The research indicates that higher stenotic degree and bilateral carotid stenosis may cause rCBF decrease in geriatric carotid stenosis. Carotid stenting may improve rCBF and change clinical symptoms significantly.
Assuntos
Encéfalo/irrigação sanguínea , Estenose das Carótidas/fisiopatologia , Stents , Idoso , Idoso de 80 Anos ou mais , Estenose das Carótidas/cirurgia , Circulação Cerebrovascular , Feminino , Seguimentos , Humanos , Masculino , Fluxo Sanguíneo Regional , Estudos RetrospectivosRESUMO
At present, cancers have been causing deadly fears to humans and previously unpredictable losses to health. Especially, lung cancer is one of the most common causes of cancer-related mortality accounting for approximately 15% of all cancer cases worldwide. While Non-Small Cell Lung Carcinomas (NSCLCs) makes up to 80% of lung cancer cases. The patient compliance has been weakening because of serious drug resistance and adverse drug effects. Therefore, there is an urgent need for the development of novel structural agents to inhibit NSCLCs. Nitrogen-containing heterocyclic compounds exhibit wide range of biological properties, especially antitumor activity. We reviewed some deadly defects of clinical medicines for the lung cancer therapy and importance of nitrogen based heterocyclic derivatives against NSCLCs. Nitrogen heterocycles exhibit significant antitumor activity against NSCLCs. Nitrogen heterocyclic hybrids could be developed as multi-target-directed NSCLC inhibitors and it is believed that the review is significant for rational designs and new ideas in the development of nitrogen heterocyclic-based drugs.
Assuntos
Antineoplásicos/química , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Compostos Heterocíclicos/química , Neoplasias Pulmonares/tratamento farmacológico , Nitrogênio/química , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Azóis/química , Azóis/farmacologia , Azóis/uso terapêutico , Carcinoma Pulmonar de Células não Pequenas/patologia , Proliferação de Células/efeitos dos fármacos , Resistencia a Medicamentos Antineoplásicos/efeitos dos fármacos , Compostos Heterocíclicos/farmacologia , Compostos Heterocíclicos/uso terapêutico , Humanos , Neoplasias Pulmonares/patologia , Piridinas/química , Piridinas/farmacologia , Piridinas/uso terapêuticoRESUMO
BACKGROUND: Vertebrobasilar artery stenosis is an important cause of ischemic posterior circulation strokes. This study aimed at evaluating the safety and efficacy of treatment including conservative therapy alone and conservative plus endovascular therapy for elderly patients with symptomatic vertebrobasilar artery stenosis. METHODS: Patients older than 60 years with symptomatic vertebrobasilar artery stenosis (> or = 50%) confirmed by cerebral angiography were enrolled. All of them were treated with medical therapy and some with additional stent-assisted angioplasty (the stenting subgroup). Their clinical, imaging, intervention and follow-up data were analyzed. RESULTS: One hundred and seventeen consecutive elderly patients (100 men, mean age (68.1 +/- 5.1) years) were enrolled and followed up for a mean time of 28.4 months; 81.7% of them were symptomatically resolved or improved; a stroke rate of 5.1% and a stroke-related death rate of 1.7% were found among them during the hospitalization and follow-up. In the stenting subgroup, 78 balloon expandable stents were employed in the 70 patients with a technical success rate of 98.7% and the mean degree of stenosis was significantly reduced from (81.7 +/- 14.3)% before stenting to (8.3 +/- 4.2)% after stenting (P < 0.001). Four (5.7%) periprocedural strokes occurred, of whom two led to death within 30 days after the procedure. During the follow-up (mean 27.7 months), sixty of the surviving 68 patients in the stenting subgroup were symptomatically resolved or improved. Only one (1.5%) posterior circulation stroke occurred, while duplex ultrasound scan of 34 patients demonstrated 10 (29.4%) in-stent restenosis. CONCLUSIONS: Appropriate utilization of conservative therapy alone and conservative plus endovascular therapy may improve short-term clinical outcomes for elderly patients with symptomatic vertebrobasilar artery stenosis. Furthermore, stent-assisted angioplasty is technically feasible and relatively safe in elderly patients.
Assuntos
Angioplastia com Balão/métodos , Stents , Insuficiência Vertebrobasilar/terapia , Idoso , Idoso de 80 Anos ou mais , Feminino , Seguimentos , Humanos , Masculino , Pessoa de Meia-Idade , Estudos Prospectivos , Resultado do TratamentoRESUMO
OBJECTIVE: To investigate the effects of microoperations combined with embolization in treatment of spinal cord hemangioblastoma. METHODS: Thirty-six patients with spinal cord hemangioblastoma, 21 males and 15 females, aged 24.2 (12-48), underwent MRI and digital abstraction angiography. Twelve of them underwent pure microsurgical treatment and 24 of them underwent operation combined with remobilization. RESULTS: MRI showed clear boundary mass, and DSA showed round or oval high density images with clear boundary and definite supplying artery. 30 cases had their tumors totally removed; and 6 cases had their tumors subtotally removed. Complete functional recovery was seen in 27 of the 36 patients (67%). Four patients resumed their self-care ability,and 4 still needed someone's help. CONCLUSION: Embolization lowers the blood supply of the spinal cord hemangioblastoma, elevates the cure rate, and enlarges the indication of spinal cord hemangioblastoma operation.
Assuntos
Embolização Terapêutica/métodos , Hemangioblastoma/terapia , Microcirurgia/métodos , Neoplasias da Medula Espinal/terapia , Adolescente , Adulto , Criança , Terapia Combinada , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Resultado do Tratamento , Adulto JovemRESUMO
OBJECTIVES: To establish a theoretical model for the tortuosity of internal carotid artery and summarize the hemodynamic rule of blood flow in a tortuous artery. To explore the relationship of cerebral ischemia and tortuous internal carotid artery. METHODS: Taking the internal carotid artery as a prototype, a geometric model of a tortuous artery was constructed according to the normal physiological and anatomical parameters of internal carotid artery. The boundary conditions and calculation conditions of blood flow are proposed. The numerical simulation of the blood flow in the tortuous artery is carried out with finite element method. Hemodynamic parameters of internal carotid artery were measured in 15 cases with the tortuosity of internal carotid artery and in 15 cases of normal control group. Blood pressure was measured by microcatheter connecting a pressure transducer at internal carotid artery, pre-tortuous and post-tortuous artery. The diameter and length of the above artery were measured and calculated by DSA machine. RESULTS: Numerical simulation results indicated pressure drop of blood flow and elongated length of artery is increased with diminution of the angle of tortuous artery. Clinical measurement data disclosed the same trend in the same curve as numerical simulation. CONCLUSION: The elongation and tortuosity of internal carotid artery results in decrease of blood pressure in the distal segment of tortuous internal carotid artery, kinking of internal carotid artery may be one of factors related to attack of cerebral ischemia on certain conditions.
Assuntos
Artéria Carótida Interna/fisiopatologia , Estenose das Carótidas/fisiopatologia , Modelos Cardiovasculares , Adulto , Idoso , Encéfalo/irrigação sanguínea , Isquemia Encefálica/etiologia , Isquemia Encefálica/fisiopatologia , Estenose das Carótidas/complicações , Feminino , Análise de Elementos Finitos , Hemodinâmica , Humanos , Masculino , Pessoa de Meia-Idade , Fluxo Sanguíneo RegionalRESUMO
OBJECTIVE: To evaluate the feasibility, safety and short-term efficacy of stent-assisted angioplasty and/or drug therapy for elderly patients with symptomatic vertebrobasilar insufficiency. METHODS: Elderly patients (> or = 60 years old) with symptomatic vertebrobasilar stenosis (> or = 50%) demonstrated by cerebral angiography were treated with drug therapy and some with endovascular stenting further from April 2001 to June 2006. The clinical, imaging, intervention and follow-up data were collected and analyzed. RESULTS: Eighty-one elderly patients were chosen for study, including 68 males and 13 females. The mean age is 70 years (60 - 87 years); stroke rate of 4.9% (4/81) and stroke-related mortality rate of 2.5% (2/81) were found in this group during hospitalization and follow-up (mean 28.1 months), and symptoms resolved or improved clinically in 66 (81.5%). Fifty-two balloon expandable stents were placed in 48 (59.3%) patients of this group with a technical success rate of 98.1% and the mean degree of stenosis was reduced from (82.4 +/- 13.1)% to (6.4 +/- 3.2)% (t = 22.4, P = 0.00). CONCLUSIONS: Appropriate management including endovascular stenting and/or drug therapy may improve short-term outcomes of elderly patients with symptomatic vertebrobasilar insufficiency; meanwhile, stent-assisted angioplasty is technically feasible and relatively safe.
Assuntos
Angioplastia com Balão , Stents , Insuficiência Vertebrobasilar/terapia , Idoso , Idoso de 80 Anos ou mais , Anticoagulantes/uso terapêutico , Feminino , Seguimentos , Humanos , Masculino , Pessoa de Meia-Idade , Inibidores da Agregação Plaquetária/uso terapêutico , Estudos Prospectivos , Resultado do Tratamento , Insuficiência Vertebrobasilar/tratamento farmacológicoRESUMO
BACKGROUND: An alarming increment in pathogenic resistance to existing anti-microbial agents is a serious problem and the treatment of these bacterial infections is becoming increasingly challenging. Therefore, there is an urgent need to develop novel antimicrobial agents. OBJECTIVE: As a part of our ongoing studies toward the development of novel antibacterial agents, the synthesis and antibacterial activity of a series of (Z)-5-((3-phenyl-1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one derivatives will be discussed in this study. METHOD: (Z)-5-((3-phenyl-1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one derivatives were designed, synthesized and evaluated for antibacterial activity. The structures were confirmed by IR, 1H NMR, 13C NMR and mass spectrometry. All of the synthesized compounds were evaluated in vitro using a 96-well microtiter plate and a serial dilution method to obtain their minimum inhibitory concentration (MIC) values against a variety of different strains, including multidrug-resistant clinical isolates. RESULTS: The antibacterial test in-vitro showed that most compounds in series 7 and 9 exhibited significant inhibitory activities against anaerobic bacteria (Streptococcus mutans) strains with a MIC value of 1 µg/mL. Compounds 7c and 9c showed the most potent activity against MRSA (3167 and 3506) with a minimum inhibitory concentration (MIC) value of 1 µg/mL, which is equivalent to moxifloxacin and greater than gatifloxacin, oxacillin and norfloxacin. Additionally, compound 9c showed potent antibacterial activity against Bacillus subtilis (aerobic bacteria) with a MIC value of 2 µg/mL. CONCLUSION: The work suggests that these type of rhodanine compounds had a better potent activity against MRSA compared with other perviously reported rhodanine derivatives, which might provide a valuable information for the development of new antibacterial agents against multidrug-resistant clinical isolates MRSA.
Assuntos
Antibacterianos/farmacologia , Pirazóis/farmacologia , Tioidantoínas/farmacologia , Antibacterianos/síntese química , Bacillus subtilis/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Farmacorresistência Bacteriana , Escherichia coli/efeitos dos fármacos , Fluoroquinolonas/farmacologia , Gatifloxacina , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Moxifloxacina , Norfloxacino/farmacologia , Oxacilina/farmacologia , Pirazóis/síntese química , Estereoisomerismo , Streptococcus mutans/efeitos dos fármacos , Tioidantoínas/síntese químicaRESUMO
OBJECTIVE: To investigate the working memory of patients with cervicocerebral artery stenosis and its change after stenting. METHODS: 35 patients with cervicocerebral artery stenosis (≥50% with related symptoms of cerebral ischemia, or ≥70% with or without related symptoms of cerebral ischemia) underwent endovascular stenting. Working memory of all 35 patients before and within 3 weeks of stenting was evaluated by memory quotient (MQ) scores. Change in regional cerebral blood flow (rCBF) was assessed by single photon emission CT (SPECT) for 13 of the patients. MQ scores were compared according to location and degree of stenosis for all patients, as well as changes in rCBF for the 13 patients. RESULTS: Mean MQ scores were significantly lower than normal for patients with carotid artery stenosis alone and for patients with carotid stenosis in addition to vertebrobasilar and/or subclavical stenosis, but not for patients with vertebrobasilar and/or subclavical stenosis. MQ scores were significantly increased after stenting for all patients, especially those with carotid stenosis. There was no significant difference between patients with moderate stenosis and those with severe (>70%) stenosis in MQ increments pre- and post-stenting (p=0.085). Nine of the 13 patients who received SPECT showed an improvement in rCBF after stenting, and their MQ increments were significantly higher than those without an improvement in rCBF (p=0.020). CONCLUSIONS: Working memory impairment can be observed in patients with cervicocerebral artery stenosis, especially those with carotid stenosis. Endovascular stenting of stenosis might improve the impairment by alleviating cerebral perfusion deficit.
Assuntos
Isquemia Encefálica/cirurgia , Estenose das Carótidas/cirurgia , Revascularização Cerebral/métodos , Transtornos da Memória/cirurgia , Memória de Curto Prazo , Stents , Idoso , Idoso de 80 Anos ou mais , Isquemia Encefálica/etiologia , Estenose das Carótidas/complicações , Circulação Cerebrovascular , Feminino , Humanos , Masculino , Transtornos da Memória/etiologia , Pessoa de Meia-Idade , Recuperação de Função Fisiológica , Resultado do TratamentoRESUMO
Two novel series of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives were designed and synthesized, and their anti-bacterial activities evaluated. These compounds showed broad-spectrum inhibitory activities against both Gram-positive and Gram-negative bacteria with minimum inhibitory concentration (MIC) values in the range of 1-64 µg/mL. The activity of compound 6c was the more potent with MIC values of 1 µg/mL against the MRSA (3167 and 3506) strains than those of gatifloxacin, oxacillin, and norfloxacin. Compared to the previously reported rhodanine derivatives, 2-thioxothiazolidin-4-one derivatives exhibited an inhibition against Gram-negative strains due to the introduction of a 1,3,4-oxadiazole moiety, among which compounds 3 showed moderate activities against the Gram-negative bacteria (Escherichiacoli 1924) with MIC values of 16 µg/mL.
Assuntos
Anti-Infecciosos/síntese química , Anti-Infecciosos/farmacologia , Tiazolidinas/síntese química , Tiazolidinas/farmacologia , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Espectrometria de Massas por Ionização e Dessorção a Laser Assistida por Matriz , Espectrofotometria InfravermelhoRESUMO
PURPOSE: Tiny intracranial aneurysms pose a significant therapeutic challenge for interventional neuroradiologists. The authors report their preliminary results of endovascular treatment of these aneurysms. METHODS: Between January 2002 and December 2009, 52 tiny intracranial aneurysms (defined as ≤ 3 mm in maximum diameter) in 46 patients (22 men; mean age, 57.9 years) were treated by endosaccular coil embolisation or sole stent deployment in the parent artery. Of 52 aneurysms, 29 had ruptured and 23 remained unruptured. The initial angiographic results, procedural complications, and clinical outcomes were assessed at discharge. Imaging follow-up was performed with cerebral angiography. RESULTS: One aneurysm coiling procedure failed because of unsuccessful micro-catheterization. Forty-three aneurysms were successfully coil embolized, of which complete occlusion was obtained in 14, subtotal occlusion in 18 and incomplete occlusion in 11. The other 8 aneurysms were treated by sole stent deployment in the parent artery. Procedural complications (2 intraprocedural ruptures and 3 thromboembolic events) occurred in 5 (9.6%) of 52 aneurysms, resulting in permanent morbidity in only 1 (2.2%, 1/46) patient. No rebleeding occurred during clinical follow-up (mean duration, 46.7 months). Of the 16 coiled aneurysms that receiving repetitive angiography, 6 initially completely and 3 subtotally occluded aneurysms remained unchanged, 4 initially subtotally and 3 incompletely occluded aneurysms progressed to total occlusion. Five sole stent deployed aneurysms received angiographic follow-up (mean duration, 10.0 months), of which 3 remained unchanged, 1 became smaller and 1 progressed to total occlusion. CONCLUSION: Endovascular treatment of tiny intracranial aneurysms is technical feasible and relatively safe. Coil embolisation seems to be effective in preventing early recanalisation, whereas sole stenting technique needs further investigation to determine its effectiveness.