Bioorganic and Medicinal Chemistry Letters p. 1973 - 1978 (1998)
Update date:2022-08-03
Topics: Derivatives In Vivo Studies In Vitro Assays Toxicity Evaluation Structure-Activity Relationship Experimental Design Pharmacokinetic analysis
Hirokawa, Yoshimi
Yamazaki, Hiroshi
Yoshida, Naoyuki
Kato, Shiro
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 of apomorphine-induced emesis in dogs) along with gastroprokinetic activity (gastric emptying in rats).
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