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

被引：15

作者：

Hirokawa, Y ^{[1
]}

Yamazaki, H ^{[1
]}

Yoshida, N ^{[1
]}

Kato, S ^{[1
]}

机构：

[1] Dainippon Pharmaceut Co Ltd, Discovery Res Labs 1, Osaka 5640053, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 15期

关键词：

D O I：

10.1016/S0960-894X(98)00341-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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). (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：1973 / 1978

页数：6