RESUMO
New acetamidines structurally related to N-(3-(aminomethyl)benzyl)acetamidine (1, W1400) were designed as inhibitors of inducible nitric oxide synthase (iNOS). Six compounds were found to be selective for iNOS over endothelial nitric oxide synthase (eNOS), and among them, the most active and selective compound was the N-benzylacetamidine 2. A docking study was also performed to shed light on the effects of the structural modifications on the interaction of the designed inhibitors with the NOS.
Assuntos
Amidinas/síntese química , Benzilaminas/síntese química , Óxido Nítrico Sintase Tipo II/antagonistas & inibidores , Amidinas/química , Benzilaminas/química , Sítios de Ligação , Modelos Moleculares , Ligação Proteica , Relação Estrutura-AtividadeRESUMO
The thiophene-, benzothiazole- and pyridine-thioaryloxyacids analogues of clofibric acid were synthesized and their antiplatelet activity was screened. Some compounds exhibited antiaggregating properties. The platelet-related haemostasis was measured on a PFA-100 analyzer using bull blood.
Assuntos
Ácido Clofíbrico/síntese química , Ácido Clofíbrico/farmacologia , Agregação Plaquetária/efeitos dos fármacos , Tiazóis/farmacologia , Animais , Bovinos , Ácido Clofíbrico/análogos & derivados , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos , Hipolipemiantes/síntese química , Hipolipemiantes/química , Hipolipemiantes/farmacologia , Tiazóis/síntese químicaRESUMO
Compounds structurally related to the known antimicrobial drug linezolid were selected in order to evaluate the influence of electron-withdrawing properties and altered geometric features as a result of the N-substituent modification. After a preliminary study of molecular modeling, cinnamoyl-, pyridin- and pyrimidinoxazolidin-2-ones were synthesized. None of the new compounds showed antibacterial activity.
