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Chem Biodivers ; 5(5): 714-28, 2008 May.
Artigo em Inglês | MEDLINE | ID: mdl-18493958

RESUMO

Two series of (+/-)-2-phenyl-1-(quinolizidin-1 alpha-yl)benzimidazoles, 12A-26A, and (+/-)-2-phenyl-1-(quinolizidin-1 beta-yl)benzimidazoles, 12B-26B, were prepared and tested for the inhibition of human platelets aggregation induced by ADP, collagen, and adrenaline. All epimers A, i.e., 12A-26A, were devoid of any activity against the three agonists, while the epimers B, i.e., 12B-26B, exhibited different degrees of activity, though practically confined against the ADP-induced aggregation. The best compounds were 19B, 24B, and 26B, which inhibited for 69-67% at 260 microM and for 40-29% at 65 microM concentration the ADP (2 microM)-induced aggregation. The observed agonist and spatial structure selectivity warrant further investigations of this kind of benzimidazole derivatives.


Assuntos
Benzimidazóis/química , Benzimidazóis/farmacologia , Plaquetas/efeitos dos fármacos , Agregação Plaquetária/efeitos dos fármacos , Quinolizidinas/química , Benzimidazóis/síntese química , Humanos , Estrutura Molecular
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