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Pharmazie ; 59(12): 899-905, 2004 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-15638075

RESUMO

In an effort to establish new antiulcer agents a series of 2-(2-substituted amino)-1 H-benzimidazoles 8, 9, 14; 1,3-disubstituted-3,4-dihydropyrimido[1,6-a]benzimidazoles 4, 7, 11, 12; 3-substituted-3,4-dihydropyrimido[1,6-a]benzimidazol-1 (2H)-thiones (or (2H)-ones) 10, 17 and 3-substituted-1,2,3,4-tetrahydropyrimido[1,6-a]benzimidazoles 15 were synthesized. Representative members were selected to evaluate their gastric antisecretory activity using an in vivo pylorus ligated rat method. Omeprazole was used as reference. The results indicated that the test compounds exhibit gastric antisecretory activity. The percent inhibition+/-SEM at the indicated dose level was demonstrated as omeprazole (59%+/-0.16 at 3 mg/kg) > 15a (53%+/-1.39 at 3 mg/kg) > 7a (51%+/-1.04 at 1 mg/kg) > 10a (50%+/-1.36 at 3 mg/kg).


Assuntos
Antiulcerosos/síntese química , Antiulcerosos/farmacologia , Benzimidazóis/síntese química , Benzimidazóis/farmacologia , Pirimidinas/síntese química , Pirimidinas/farmacologia , Animais , Peso Corporal , Mucosa Gástrica/efeitos dos fármacos , Mucosa Gástrica/metabolismo , Indicadores e Reagentes , Masculino , Omeprazol/farmacologia , Piloro/fisiologia , Ratos , Relação Estrutura-Atividade
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