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1.
J Enzyme Inhib Med Chem ; 34(1): 333-342, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30734600

RESUMO

Leishmaniasis is considered as one of the major neglected tropical diseases due to its magnitude and wide geographic distribution. Leishmania braziliensis, responsible for cutaneous leishmaniasis, is the most prevalent species in Brazil. Superoxide dismutase (SOD) belongs to the antioxidant pathway of the parasites and human host. Despite the differences between SOD of Leishmania braziliensis and human make this enzyme a promising target for drug development efforts. No medicinal chemistry effort has been made to identify LbSOD inhibitors. Herein, we show that thermal shift assays (TSA) and fluorescent protein-labeled assays (FPLA) can be employed as primary and secondary screens to achieve this goal. Moreover, we show that thiazole derivatives bind to LbSOD with micromolar affinity.


Assuntos
Inibidores Enzimáticos/farmacologia , Leishmania braziliensis/enzimologia , Superóxido Dismutase/antagonistas & inibidores , Tiazóis/farmacologia , Brasil , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Humanos , Estrutura Molecular , Relação Estrutura-Atividade , Superóxido Dismutase/metabolismo , Tiazóis/síntese química , Tiazóis/química
2.
Braz J Microbiol ; 55(2): 1811-1816, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38739216

RESUMO

As the prevalence of drug-resistant Candida isolates continues to rise, the imperative for identifying novel compounds to enhance the arsenal of antifungal drugs becomes increasingly critical. Consequently, exploring new treatment strategies, including synthesizing molecular hybrids and applying combination therapy, is essential. For this reason, this study evaluated the efficacy of ten molecular hybrids of aza-bicyclic 2-isoxazoline-acylhydrazone belonging to two series 90 and 91 as possible anti-Candida agents. In addition, we also investigated the interaction between the hybrids and fluconazole, a commonly used antifungal drug. We evaluated the antifungal effect of aza-bicyclic 2-isoxazoline-acylhydrazone hybrid compounds against six Candida spp. strains that target planktonic cells. However, none of these new molecules were inhibitory active at the tested concentrations (2 to 1,024 µg/mL). Moreover, we analyzed the interaction between the ten new hybrid molecules and fluconazole using the checkerboard assay, employing two different methodologies for reading the plate. For this, one isolate fluconazole-resistant was selected. We observed that only one combination, 6-(4-tert-butylbenzoil)-4,5,6,6a-tetrahydro-3a-H-pirrole[3,2-d]isoxazole-3-carboxylic(furan-2-metilidene)-hydrazide (91e) and fluconazole, exhibited a synergistic interaction (FICI range 0.0781 to 0.4739). The combination successfully inhibited the growth of C. albicans CA2 fluconazole-resistant, and no interaction was observed in an isolate susceptible to fluconazole. Additionally, these results emphasize the continued need for research into new compounds and the importance of using combined approaches to increase their activity.


Assuntos
Antifúngicos , Candida albicans , Farmacorresistência Fúngica , Sinergismo Farmacológico , Fluconazol , Hidrazonas , Isoxazóis , Testes de Sensibilidade Microbiana , Antifúngicos/farmacologia , Antifúngicos/química , Fluconazol/farmacologia , Candida albicans/efeitos dos fármacos , Hidrazonas/farmacologia , Hidrazonas/química , Isoxazóis/farmacologia , Isoxazóis/química , Humanos
3.
BMC Emerg Med ; 13: 2, 2013 Jan 29.
Artigo em Inglês | MEDLINE | ID: mdl-23360089

RESUMO

BACKGROUND: Identification of delirium in emergency departments (ED) is often underestimated; within EDs, studies on delirium assessment and relation with patient outcome in Intermediate Care Units (IMCU) appear missing in European hospital settings. Here we aimed to determine delirium prevalence in an EDIMCU (Hospital de Braga, Braga, Portugal) and assessed routine biochemical parameters that might be delirium indicators. METHODS: The study was prospective and observational. Sedation level was assessed via the Richmond Agitation-Sedation Scale and delirium status by the Confusion Assessment Method for the ICU. Information collected included age and gender, admission type, Charlson Comorbidity Index combined condition score (Charlson score), systemic inflammatory response syndrome criteria (SIRS), biochemical parameters (blood concentration of urea nitrogen, creatinine, hemoglobin, sodium and potassium, arterial blood gases, and other parameters as needed depending on clinical diagnosis) and EDIMCU length of stay (LOS). Statistical analyses were performed as appropriate to determine if baseline features differed between the 'Delirium' and 'No Delirium' groups. Multivariate logistic regression was performed to assess the effect of delirium on the 1-month outcome. RESULTS: Inclusion and exclusion criteria were met in 283 patients; 238 were evaluated at 1-month for outcome follow-up after EDIMCU discharge ("good" recovery without complications requiring hospitalization or institutionalization; "poor" institutionalization in permanent care-units/assisted-living or death). Delirium was diagnosed in 20.1% patients and was significantly associated with longer EDIMCU LOS. At admission, Delirium patients were significantly older and had significantly higher blood urea, creatinine and osmolarity levels and significantly lower hemoglobin levels, when compared with No Delirium patients. Delirium was an independent predictor of increased EDIMCU LOS (odds ratio 3.65, 95% CI 1.97-6.75) and poor outcome at 1-month after discharge (odds ratio 3.51, CI 1.84-6.70), adjusted for age, gender, admission type, presence of SIRS criteria, Charlson score and osmolarity at admission. CONCLUSIONS: In an EDIMCU setting, delirium was associated with longer LOS and poor outcome at 1-month post-discharge. Altogether, findings support the need for delirium screening and management in emergency settings.


Assuntos
Delírio/epidemiologia , Serviço Hospitalar de Emergência , Instituições para Cuidados Intermediários , Distribuição por Idade , Idoso , Comorbidade , Creatinina/sangue , Delírio/diagnóstico , Feminino , Hemoglobinas/análise , Mortalidade Hospitalar , Humanos , Institucionalização/estatística & dados numéricos , Tempo de Internação/estatística & dados numéricos , Masculino , Pessoa de Meia-Idade , Análise Multivariada , Concentração Osmolar , Portugal/epidemiologia , Estudos Prospectivos , Síndrome de Resposta Inflamatória Sistêmica/epidemiologia , Ureia/sangue
4.
Rev Port Cardiol ; 32(3): 253-6, 2013 Mar.
Artigo em Português | MEDLINE | ID: mdl-23317686

RESUMO

We present a case of acute heart failure as the first manifestation of Graves' disease. It illustrates some of its cardiovascular complications, particularly atrial fibrillation, pulmonary hypertension and heart failure. This case report highlights the importance of considering hyperthyroidism as a cause of idiopathic pulmonary hypertension, and demonstrates the potential reversibility of its complications.


Assuntos
Insuficiência Cardíaca/complicações , Hipertensão Pulmonar/complicações , Hipertireoidismo/complicações , Adulto , Feminino , Humanos
5.
Future Microbiol ; 18: 1225-1233, 2023 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-37882752

RESUMO

Aim: To evaluate antifungal potential of 5,6,7,8-tetrahydroimidazo[1,2-a]pyrazine hybrids based on thiosemicarbazones and thiazolidinediones against pathogenic Sporothrix species. Methods: Antifungal activity of nine compounds were assessed by broth microdilution. Interactions between active compounds and itraconazole were evaluated by the checkerboard assay using non-wild-type isolates. Cytotoxicity of the compounds was determined. Results: Four C-3 substituted analogs showed antifungal activity, unrelated to thiosemicarbazone or thiazolidinedione functions. Synergistic interactions between the four compounds and itraconazole, and low toxicity on mouse fibroblast cells were observed. Activity of 5,6,7,8-tetrahydroimidazo[1,2-a]pyrazine hybrids against Sporothrix depended on the substitution on the imidazopyrazine ring. Conclusion: Antifungal potential, overcoming itraconazole resistance and low toxicity indicate the possible use of that series of compounds in a therapeutic alternative for treatment of sporotrichosis.


Assuntos
Sporothrix , Tiazolidinedionas , Tiossemicarbazonas , Animais , Camundongos , Antifúngicos/farmacologia , Itraconazol/farmacologia , Tiossemicarbazonas/farmacologia , Testes de Sensibilidade Microbiana
6.
Curr Top Med Chem ; 22(4): 247-258, 2022 Mar 04.
Artigo em Inglês | MEDLINE | ID: mdl-34986770

RESUMO

BACKGROUND: In a study recently published by our research group, the isoxazoline-acylhydrazone derivatives R-99 and R-123 presented promising antinociceptive activity. However, the mechanism of action of this compound is still unknown. OBJECTIVE: This study aimed to assess the mechanisms involved in the antinociceptive activity of these compounds in chemical models of pain. METHODS: Animals were orally pretreated and evaluated in the acetic acid-, formalin-, capsaicin-, carrageenan- and Complete Freund's Adjuvant (CFA)-induced pain models in mice. The effects of the compounds after pretreatment with naloxone, prazosin, yohimbine, atropine, L-arginine, or glibenclamide were studied, using the acetic acid-induced writhing test to verify the possible involvement of opioid, α1-adrenergic, α2-adrenergic or cholinergic receptors, and nitric oxide or potassium channels pathways, respectively. RESULTS: R-99 and R-123 compounds showed significant antinociceptive activity on pain models induced by acetic acid, formalin, and capsaicin. Both compounds decreased the mechanical hyperalgesia induced by carrageenan or CFA in mice. The antinociceptive effects of R-99 and R-123 on the acetic acid-induced writhing test were significantly attenuated by pretreatment with naloxone, yohimbine or atropine. R-99 also showed an attenuated response after pretreatment with atropine and glibenclamide. However, on the pretreatment with prazosin, there was no change in the animals' response to both compounds. CONCLUSION: R-99 and R-123 showed antinociceptive effects related to mechanisms that involve, at least in part, interaction with the opioid and adrenergic systems and TRPV1 pathways. The compound R-99 also interacts with the cholinergic pathways and potassium channels.


Assuntos
Analgésicos , Nociceptividade , Analgésicos/farmacologia , Analgésicos/uso terapêutico , Analgésicos Opioides/efeitos adversos , Animais , Camundongos , Dor/tratamento farmacológico , Extratos Vegetais/química
7.
Theor Biol Forum ; 112(1-2): 101-107, 2019 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-32125354

RESUMO

1. The Position of Suzan Mazur. 2. The Interviews with over 25 Scientists. 3. What is Darwinism and Neo-Darwinism. 4. The Positive Contribution of Darwinism. 5. The Negative Aspects of Darwinism. 6. A View into Future Research that Will Allow the Unraveling of the Mechanism of Evolution. 7. A Final Note.


Assuntos
Evolução Biológica , Seleção Genética
8.
Pharmaceuticals (Basel) ; 12(4)2019 Nov 17.
Artigo em Inglês | MEDLINE | ID: mdl-31744203

RESUMO

Fourteen arylsemicarbazone derivatives were synthesized and evaluated in order to find agents with potential anticancer activity. Cytotoxic screening was performed against K562, HL-60, MOLT-4, HEp-2, NCI-H292, HT-29 and MCF-7 tumor cell lines. Compounds 3c and 4a were active against the tested cancer cell lines, being more cytotoxic for the HL-60 cell line with IC50 values of 13.08 µM and 11.38 µM, respectively. Regarding the protein kinase inhibition assay, 3c inhibited seven different kinases and 4a strongly inhibited the CK1δ/ε kinase. The studied kinases are involved in several cellular functions such as proliferation, migration, cell death and cell cycle progression. Additional analysis by flow cytometry revealed that 3c and 4a caused depolarization of the mitochondrial membrane, suggesting apoptosis mediated by the intrinsic pathway. Compound 3c induced arrest in G1 phase of the cell cycle on HL-60 cells, and in the annexin V assay approximately 50% of cells were in apoptosis at the highest concentration tested (26 µM). Compound 4a inhibited cell cycle by accumulation of abnormal postmitotic cells at G1 phase and induced DNA fragmentation at the highest concentration (22 µM).

9.
Medchemcomm ; 10(11): 1916-1925, 2019 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-32133104

RESUMO

The aim of this study was to investigate the anti-inflammatory effects of two new isoxazoline-acylhydrazone derivatives: N'-(4-methoxybenzylidene)-6-(4-nitro-benzoyl)-3a,5,6,6a-tetrahydro-4H-pyrrolo[3,2-d]isoxazole-3-carbohydrazide (R-123) and N'-(4-chlorobenzylidene)-6-(4-chlorobenzoyl)-3a,5,6,6a-tetrahydro-4H-pyrrolo[3,2-d]isoxazole-3-carbohydrazide (R-99). An air pouch induced by carrageenan was used for screening the best dose of R-99 and R-123. Using this mouse model, leukocyte migration and cytokine levels (TNF-α and IL-1ß) were determined. Paw edema induced by several phlogistic agents and vascular permeability induced by acetic acid were employed to investigate the mechanism of action of the isoxazoline-acylhydrazone derivatives. A docking study was performed with the human histamine H1 receptor to investigate potential antihistaminic activity. Treatment with the compounds reduced leukocyte migration in the air pouch at all doses tested. TNF-α and IL-1ß levels were similarly reduced by the two compounds. Vasoactive amines were inhibited in models of paw edema induced by several agents and vascular permeability induced by acetic acid. The docking study suggests that R-99 and R-123 may be inhibitors of the histamine H1 receptor. In conclusion, the results indicate that R-99 and R-123 exhibit promising anti-inflammatory activity related to their ability to inhibit TNF-α, IL-1ß, and vasoactive amine production, as well as reduce leukocyte migration and inhibit mast cell degranulation.

10.
Bioorg Med Chem ; 16(1): 446-56, 2008 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-17905587

RESUMO

In the present communication, a new series of 2-[(phenylmethylene)hydrazono]-4-oxo-3-phenyl-5-thiazolidineacetic acids (2a-p) have been synthesized. Benzaldehyde 4-phenyl-3-thiosemicarbazones substituted (1a-p) were also obtained and used as intermediate to give the title compounds. All synthesized compounds were characterized by IR, (1)H and (13)C NMR. The in vitro anti-Toxoplasma gondii activity of 1a-p and 2a-p was evaluated. The 4-thiazolidinones (2a-p) were screened for their in vitro antimicrobial activity. For anti-Toxoplasma gondii activity, in general, all compounds promoted decreases in the percentage of infected cells leading to parasite elimination. These effects on intracellular parasites also caused a decrease in the mean number of tachyzoites. In addition, most of the 4-thiazolidinones showed more effective toxicity against intracellular parasites, with IC(50) values ranging from 0.05 to 1 mM. According to results of antimicrobial activity, compounds 2f, 2l, and 2p showed best activity against Mycobacterium luteus, 2c was more active against Mycobacterium tuberculosis, and 2g, 2l, and 2n showed same activity as nistatin (standard drug) against Candida sp. (4249).


Assuntos
Anti-Infecciosos/síntese química , Antiprotozoários/síntese química , Tiazolidinas/síntese química , Tiossemicarbazonas/síntese química , Toxoplasma/efeitos dos fármacos , Animais , Anti-Infecciosos/farmacologia , Antiprotozoários/farmacologia , Candida/efeitos dos fármacos , Humanos , Concentração Inibidora 50 , Mycobacterium/efeitos dos fármacos , Mycobacterium tuberculosis/efeitos dos fármacos , Análise Espectral , Tiazolidinas/farmacologia , Tiossemicarbazonas/farmacologia
11.
J Endod ; 44(5): 703-710, 2018 May.
Artigo em Inglês | MEDLINE | ID: mdl-29571913

RESUMO

INTRODUCTION: Endodontic pain is a symptom of pulpal and/or periapical inflammation. One strategy for pain reduction is using medications, such as dexamethasone. A definitive protocol for preventing and controlling pain caused by irreversible pulpitis during endodontic treatment has not yet been established. This is a systematic review to answer the following question: is the use of dexamethasone effective in controlling pain associated with symptomatic irreversible pulpitis? METHODS: This study was registered in the PROSPERO database (CRD42017058704), and Preferred Reporting Items for Systematic Reviews and Meta-Analyses statement recommendations were followed. MEDLINE, Scopus, ScienceDirect, Web of Science, Latin American Caribbean Health Sciences Literature, Cochrane Library, and Google Scholar databases were used in our research. No restrictions were applied to dates or language of publication. All records identified electronically were organized and evaluated by 2 independent authors, and, in case of doubt, a third author made the decision. The Cochrane Collaboration tool was used. The data were analyzed with RevMan 5 software (The Cochrane Collaboration, Copenhagen, Denmark), and data from eligible studies were dichotomous (with and without pain). RESULTS: A total of 4825 studies were identified. After screening, 523 studies were selected, and, after careful evaluation, only 5 articles remained. All meta-analyses revealed a global effect (P < .05, P < .05, and P < .05), which means that 4 mg dexamethasone helps relieve pain, sometimes for up to 8, 12, and 24 hours. CONCLUSIONS: The pain felt by patients diagnosed with symptomatic irreversible pulpitis may be alleviated by administering 4 mg dexamethasone either by mouth or through intraligamentary and mainly supraperiosteal injections into the root canal for up to 24 hours.


Assuntos
Anti-Inflamatórios/uso terapêutico , Dexametasona/uso terapêutico , Manejo da Dor/métodos , Pulpite/complicações , Odontalgia/tratamento farmacológico , Humanos , Medição da Dor , Pulpite/tratamento farmacológico , Odontalgia/etiologia
12.
Theor Biol Forum ; 109(1-2): 101-110, 2016 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-29513355

RESUMO

INCIPIT: It may sound as a truism but it may be necessary to recall that science is not made by instruments, or by well equipped laboratories, but by the unique personalities that use them. As a consequence their intellect, their emotional experiences and their physical ability, cannot be separated from their achievements - being they minor or profound.


Assuntos
Cromossomos/genética , Evolução Molecular , Variação Genética , Ciência , Animais , Citogenética/métodos , Citogenética/tendências , DNA/genética , Replicação do DNA , Humanos
13.
Eur J Med Chem ; 123: 639-648, 2016 Nov 10.
Artigo em Inglês | MEDLINE | ID: mdl-27517809

RESUMO

Leishmania major, as other protozoan parasites, plague human kind since pre-historic times but it remains a worldwide ailment for which the therapeutic arsenal remains scarce. Although L. major is pteridine- and purine-auxotroph, well-established folate biosynthesis inhibitors, such as methotrexate, have poor effect over the parasite survival. The lack of efficiency is related to an alternative biochemical pathway in which pteridine reductase 1 (PTR1) plays a major role. For this reason, this enzyme has been considered a promising target for anti-leishmanial drug development and several inhibitors that share the substrate scaffold have been reported. In order to design a novel class of PTR1 inhibitors, we employed the thiazolidinone ring as a bioisosteric replacement for pteridine/purine ring. Among seven novel thiazolidine-2,4-dione derivatives reported herein, 2d was identified as the most promising lead by thermal shift assays (ΔTm = 11 °C, p = 0,01). Kinetic assays reveal that 2d has IC50 = 44.67 ± 1.74 µM and shows a noncompetitive behavior. This information guided docking studies and molecular dynamics simulations (50 000 ps) that supports 2d putative binding profile (H-bonding to Ser-111 and Leu-66) and shall be useful to design more potent inhibitors.


Assuntos
Descoberta de Drogas , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Leishmania major/enzimologia , Oxirredutases/antagonistas & inibidores , Tiazolidinedionas/química , Tiazolidinedionas/farmacologia , Modelos Moleculares , Oxirredutases/química , Conformação Proteica
14.
Arq Neuropsiquiatr ; 61(3A): 621-4, 2003 Sep.
Artigo em Português | MEDLINE | ID: mdl-14513169

RESUMO

OBJECTIVE: An analysis was conducted on the etiology and the morbi-mortality of pediatric patients in acute coma, hospitalized at the Intensive Care Unit of Hospital Infantil Pequeno Príncipe (UTI-HIPP). METHOD: One hundred and four control sheets of children hospitalized at the UTI-HIPP and diagnosed as being in acute coma were analyzed. The Glasgow coma scale duly modified for children was used, with a score count equal to or lower than 8 points. The observation period was from March/98 to January/2001. All the supplementary exams as well as the neurological conditions of the patients when discharged were analyzed. RESULTS: The study comprised 104 children whose ages varied from 2 months to 13 years, with 57 (54.8%) of them being males. Hospital - stay time varied from 1 to 114 days, plus 3 cases in a persistent vegetative condition. As regards to etiology, 31 (29.8%) of the cases were due to meningo-encephalitis, 24 (23.1%) to an epileptic condition, 19 (18.3%) were toxic-metabolic, 16 (15.4%) to intra-cranial hypertension, 7 (6.7%) to shock/anoxia, 4 (3.8%) to an indeterminate etiology and 3(2.9%) were miscellaneous. Insofar as the clinical evolution of the children is concerned, 23 (22.1%) died, 32 (30.8%) evolved without any sequelae, 39 (37.5%) were discharged with neurological sequelae and for 10 (9.6%), no information is available. CONCLUSION: According to this study, one third of the children has died, one third presented neurological sequelae, and one third presented no further complications.


Assuntos
Coma/mortalidade , Adolescente , Brasil/epidemiologia , Criança , Pré-Escolar , Coma/etiologia , Feminino , Humanos , Lactente , Masculino , Estudos Retrospectivos , Taxa de Sobrevida
15.
Biomed Res Int ; 2014: 316082, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24895565

RESUMO

Antibiotic resistance is considered one of the world's major public health concerns. The main cause of bacterial resistance is the improper and repeated use of antibiotics. To alleviate this problem, new chemical substances against microorganisms are being synthesized and tested. Thiazolidines are compounds having many pharmacological activities including antimicrobial activities. For this purpose some thiazolidine derivatives substituted at position 5 in the thiazolidine nucleus were synthesized and tested against several microorganisms. Using a disc diffusion method, antimicrobial activity was verified against Gram-positive, Gram-negative, and alcohol acid resistant bacteria and yeast. The minimum inhibition concentrations (MIC) and minimum bactericidal concentrations (MBC) were determined. All derivatives showed antimicrobial activity mainly against Gram-positive bacteria, with MIC values ranging from 2 to 16 µg/mL.


Assuntos
Anti-Infecciosos/administração & dosagem , Anti-Infecciosos/síntese química , Fenômenos Fisiológicos Bacterianos/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Tiazolidinas/administração & dosagem , Tiazolidinas/síntese química , Relação Dose-Resposta a Droga , Dose Letal Mediana
16.
Rev Bras Ortop ; 45(3): 236-40, 2010.
Artigo em Inglês | MEDLINE | ID: mdl-27022547

RESUMO

OBJECTIVES: To assess the relationship between sagittal collapse, posterior instrumentation failure and the McCormack classification among patients with thoracolumbar burst fractures who had undergone posterior arthrodesis more than one level above and one level below the fracture. METHODS: This was a retrospective review based on the medical records and radiographs of 26 patients who underwent operations between January 1990 and December 2006. The parameters assessed were: worsening of kyphosis (Cobb), neurological dysfunction (Frankel) and failure of surgical treatment (implant breakage or loosening). RESULTS: No relationship was found between sagittal collapse and the scoring in the McCormack classification (r = 0.221; P = 0.322). There was also no relationship between failure of the posterior implant and the scoring in this classification (p = 0.85). CONCLUSION: Our findings suggest that this classification is not applicable to patients who underwent arthrodesis more than one level above and one level below the fracture.

17.
Eur J Med Chem ; 45(9): 3685-91, 2010 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-20541294

RESUMO

In this work we reported the synthesis and evaluation of anti-Toxoplasma gondii and antimicrobial activities in vitro of three new compound series obtained from ethyl(5-methyl-1-H-imidazole-4-carboxylate): acylthiosemicarbazide analogues 3a-d, 4-thiazolidinone analogues 4a-d and 1,3,4-thiadiazole analogues 5a-d. All synthesized compounds were characterized by IR, (1)H, (13)C NMR and HRMS. The majority of the tested compounds show excellent anti-T. gondii activity when compared to hydroxyurea and sulfadiazine. In addition it was also shown that most of the compounds in this study have a better performance against intracellular tachyzoites. The results for antimicrobial activity evaluation showed weak antibacterial and antifungal activities for all the tested molecules, when compared with the standard drugs (chloramphenicol and rifampicin for antibacterial activity; nistatin and ketoconazole for antifungal activity).


Assuntos
Semicarbazidas/síntese química , Semicarbazidas/farmacologia , Tiazolidinas/síntese química , Tiazolidinas/farmacologia , Toxoplasma/efeitos dos fármacos , Animais , Anti-Infecciosos/síntese química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antiprotozoários/síntese química , Antiprotozoários/química , Antiprotozoários/farmacologia , Bactérias/efeitos dos fármacos , Chlorocebus aethiops , Resistência a Medicamentos , Fungos/efeitos dos fármacos , Espaço Intracelular/efeitos dos fármacos , Espaço Intracelular/parasitologia , Testes de Sensibilidade Microbiana , Semicarbazidas/química , Tiazolidinas/química , Toxoplasma/fisiologia , Células Vero
18.
ROBRAC ; 20(52)abr. 2011. ilus
Artigo em Português | LILACS | ID: lil-609185

RESUMO

O preparo do canal radicular tem sido avaliado por diferentes métodos ao longo dos anos: a microscopia ótica, a microscopia eletrônica de varredura, o exame radiográfico, analises fotográficas, moldagem, os métodos computadorizados e recentemente a análise tomográfica. Até 1987, a grande dificuldade na avaliação estava na ausência de um controle negativo uma vez que o preparo só podia ser avaliado após a instrumentação. Neste ano, Bramante et al. desenvolveram um método que permitiu a análise antes e após o preparo, usando dentes incluídos em resina e em morsa adequada e seccionados transversalmente, o qual se tornou o mais importante método para análise da qualidade do preparo do canal radicular. Em 1991 Sydney et al.3, desenvolveram uma plataforma radiográfica com a finalidade de padronizar as tomadas radiográficas, obtendo numa mesma película as imagens dos instrumentos antes e depois da instrumentação, para em seguida analisar a manutenção do trajeto original do canal radicular ou não. Face às restrições no uso de dentes naturais e as dificuldades de sua obtenção, o ensino básico da endodontica viu-se obrigado a buscar alternativas. Dente estas, o uso de canais simulados tem se mostrado uma opção de grande valia o que gerou ao desenvolvimento de uma plataforma radiográfica específica para estes, tornando-se valioso auxiliar no ensino da Endodontia.


Root canal preparation has been evaluated by different methods along the years: common optical microscope, the scanning electron microscope, radiographic examination, photographic studies, root canal models, computer programs and recently the tomography. Until 1987 the difficulty on analyzing root canal preparation was the negative control. In this year, Bramante et al. introduced a method that allowed the analysis before, during and after instrumentation. In 1991 Sydney et al.3 developed the radiographic platform method that makes possible to get in the same film the position of the file at the beginning and at the end of instrumentation. Deviations and imperfection are directly observed. The importance of simulated root canals in teaching endodontics is significant as we have difficulties and restrictions on getting human tooth for the grad students. The development of a radiographic platform for simulated root canals is an important teaching aid in endodontics.

19.
GED gastroenterol. endosc. dig ; 30(3): 123-124, jul.-set. 2011. ilus
Artigo em Português | LILACS | ID: lil-678917

RESUMO

A gastrite atrófica é uma afecção gástrica relativamente frequente, principalmente na população acima dos 60 anos, e se caracteriza por um adelgaçamento da parede gástrica (especialmente da mucosa) que cursa com redução na secreção ácida. A atrofia gástrica é uma causa frequente de anemia por redução na produção de fator intrínseco, o que diminui a absorção de vitamina B12. Além disso, ela pode evoluir para neoplasia gástrica conforme proposto por Pelayo-Correa: infecção pelo H. pylori - gastrite atrófica - metaplasia intestinal - câncer gástrico (adenocarcinoma gástrico tipo intestinal de Lauren). Endoscopicamente, a gastrite atrófica se caracteriza por redução do pregueado gástrico e visualização dos vasos sanguíneos submucosos por transparência. A cromoscopia com vermelho congo é um método rápido, de fácil interpretação e baixo custo, que pode auxiliar no diagnóstico de gastrite atrófica. Trata-se de um corante que tem originalmente cor vermelha, mas que se torna negro em meio ácido. Desta forma, a mucosa secretora de ácido fica revestida por corante enegrecido, enquanto a não-secretora por corante vermelho.


Assuntos
Humanos , Feminino , Idoso , Gastrite Atrófica
20.
Rev. bras. ortop ; 45(3): 236-240, maio-jun. 2010. ilus, graf, tab
Artigo em Português | LILACS | ID: lil-555949

RESUMO

OBJETIVOS: Verificar a associação entre o colapso sagital, falha da instrumentação posterior e a classificação de McCormack nos portadores de fratura toracolombar tipo explosão submetidos à artrodese posterior maior do que um nível acima e um abaixo da fratura. MÉTODOS: Estudo retrospectivo com base em prontuários e radiografias de 22 pacientes operados entre janeiro de 1990 e dezembro de 2006. Os parâmetros avaliados foram: piora da cifose (Cobb), disfunção neurológica (Frankel) e falha do tratamento cirúrgico (quebra ou soltura do implante). RESULTADOS: Não houve correlação entre o colapso sagital e a pontuação da classificação de McCormack (r = 0,221; P = 0,322). Verificamos ainda inexistência de associação entre a falha do implante posterior e a pontuação desta classificação (p = 0,85). CONCLUSÃO: Nossos achados sugerem a falta de aplicabilidade desta classificação em pacientes submetidos a artrodese posterior maior do que um nível acima e um abaixo da fratura.


OBJECTIVES: To assess the relationship between sagittal collapse, implant failure and load sharing classification of patients suffering a thoracolumbar burst fracture treated with posterior instrumentation. METHODS: Retrospective review of radiographs and medical records of 26 patients operated on between January 1990 and December 2006. Kyphotic worsening (Cobb), neurologic dysfunction (Frankel) and the failure of surgical treatment (implant breaking or loosening) were studied. RESULTS: No relationship was found between kyphotic deformity and higher scores in the load sharing classification (r = 0,221; P = 0,322). No relationship was found between implant failure and this classification. (p = 0.85). CONCLUSION: Our findings suggest that this classification is not applicable in patients with an arthrodesis larger than one unit above and below the fracture.


Assuntos
Humanos , Masculino , Feminino , Fraturas da Coluna Vertebral , Resultado do Tratamento , Vértebras Torácicas/lesões , Suporte de Carga
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