RESUMO
A series of novel diethyl 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate embedded triazole and mannich bases were synthesized, and evaluated for their angiotensin converting enzyme (ACE) inhibitory activity. Screening of above synthesized compounds for ACE inhibition showed that triazoles functionalized compounds have better ACE inhibitory activity compared to that of mannich bases analogues. Among all triazoles we found 6 h, 6 i and 6 j to have good ACE inhibition activity with IC50 values 0.713 µM, 0.409 µM and 0.653 µM, respectively. Among mannich bases series compounds, only 7c resulted as most active ACE inhibitor with IC50 value of 0.928 µM.
Assuntos
Inibidores da Enzima Conversora de Angiotensina/síntese química , Bases de Mannich/química , Peptidil Dipeptidase A/química , Triazóis/química , Inibidores da Enzima Conversora de Angiotensina/química , Inibidores da Enzima Conversora de Angiotensina/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Di-Hidropiridinas/química , Ativação Enzimática/efeitos dos fármacos , Células HEK293 , Humanos , Bases de Mannich/síntese química , Bases de Mannich/farmacologia , Peptidil Dipeptidase A/metabolismo , Ligação Proteica , Triazóis/síntese química , Triazóis/farmacologiaRESUMO
A series of novel 2-(1H-indol-3-yl)-N-(3, 4-diphenylthiazol-2(3H)-ylidene) ethanamine derivatives (5a-o) were synthesized by cyclization of corresponding 1-(2-(1H-indol-3-yl) ethyl)-3-phenylthiourea 3 with 2-bromoacetophenone. All synthesized compounds were evaluated for in vitro antibacterial activity using Gram-positive bacteria and Gram-negative bacteria. In vitro antifungal activity also determined against the five fungal species. Structures of the synthesized compounds were established by elemental analysis and spectral data.
Assuntos
Anti-Infecciosos/síntese química , Anti-Infecciosos/farmacologia , Tiazóis/síntese química , Tiazóis/farmacologia , Anti-Infecciosos/química , Bactérias/efeitos dos fármacos , Técnicas de Química Sintética , Fungos/efeitos dos fármacos , Tiazóis/químicaRESUMO
A new series of isoxazoles and triazoles linked 2-phenyl benzothiazole were synthesized and evaluated for their anticancer activity. These compounds have been tested for their cytotoxicity three cancer cell lines. Among the compounds tested, compound 5d showed good cytotoxicity against Colo-205 and A549 cells in comparison to standard control PMX 610(1). Further compound 5d has been tested for its apoptotic activity and its inhibitory activity against caspase and PARP proteins. Hence this compound has the potential that it can be selected for further biological studies.