A novel series of 6-methoxy-1H-benzotriazole-5-carboxamide derivatives with dual antiemetic and gastroprokinetic activities

Y Hirokawa, H Yamazaki, N Yoshida, S Kato

Index: Hirokawa, Yoshimi; Yamazaki, Hiroshi; Yoshida, Naoyuki; Kato, Shiro Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 15 p. 1973 - 1978

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Citation Number: 15

Abstract

A novel series of 6-methoxy-1H-benzotriazole-5-carboxamide derivatives with a medium perhydroazacycle ring in the amine moiety were prepared, and their antiemetic and gastroprokinetic activities were evaluated. Among them, N-(1-ethylhexahydroazepin-3-yl)-, N-(1-ethyloctahydroazocin-3-yl)-and N-(1-ethyloctahydroazonin-3-yl)-6-methoxy-1H- benzotriazole-5-carboxamides (24, 36, 37) showed a potent antiemetic activity (inhibition ...