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).
View MoreWuhan Better Organic Technology Inc.
Contact:13307163183
Address:Wuhan Economic&Technology Development Zone, Hubei
Zhejiang Kangfeng Chemical Co.,LTD.
Contact:+86-579-86709687
Address:Xueshizhai Industrial Zone, Weishan Town,Dongyang City, Zhejiang Province ,China
Contact:0512-63006287
Address:no.88.YISHENG Road,etdz-WUJIANG,SUZHOU,CHINA
Shanghai Egoal Chemical Co.,Ltd
Contact:+86-21-50333091
Address:Yangming Garden Square 3,YangGao North Road 1188, Pudong New District, Shanghai
Contact:+86 512 6287 2180
Address:398 Ruoshui Road, Suzhou Industrial Park, Suzhou, Jiangsu, P. R. China
Doi:10.1016/j.carres.2020.108080
(2020)Doi:10.1021/ja01642a039
(1954)Doi:10.1021/jo302795w
(2013)Doi:10.1007/BF00513870
(1984)Doi:10.1016/j.tet.2006.06.021
(2006)Doi:10.1021/ol061029w
(2006)
