Journal of Medicinal Chemistry p. 3159 - 3164 (1991)
Update date:2022-09-26
Topics: In vitro Derivatives in vivo Potential Anticonvulsant
Calderon
Newman
Tortella
A series of analogues based on the anticonvulsant carbetapentane (1, 2-[2- (diethylamino)ethoxy]ethyl 1-phenyl-1-cyclopentylcarboxylate) was prepared as potential novel anticonvulsant drugs. Structure-activity relationships of analogues in which the ester function and cyclopentane moieties were modified have been investigated by evaluating their ability to prevent seizures in the rat maximal electroshock test. These compounds (11, ED50 = 16 μmol/kg; 12, ED50 = 86 μmol/kg, and 23, ED50 = 173 μmol/kg) were effective anticonvulsants. Compound 11, an alkyl ether derivative of 1, was more potent than the parent compound (ED50 = 48 μmol/kg) and also showed a 2-fold increase in potency compared to that of the prototypic anticonvulsant drug diphenylhydantoin.
View MoreBeijing Apis Biotechnology Co., Ltd.
Contact:86-010-67856775-8551
Address:NO.4PUHUANGYU ROAD,FENTAI DISTRICT, BEIJING, CHINA
Shandong Zhongcheng Barium Salt Co., Ltd
Contact:+86-15725732638
Address:No.29 baoxi road, hi-tech zone, zibo, shandong
Jiangsu Hualun Chemical Industry Co., Ltd
website:http://www.hualunchem.com
Contact:+86-0514-86464168 86507985
Address:39# Middle Renmin Road, Dinghuo Town
FUJIAN SHANSHUI CHEMICAL CORP.LTD.
Contact:+86-151-59920036
Address:Jinqiao Gareden, jo@fj-xinyi.com
Jinan Hongfangde Pharmatech Co.LTD
Contact:0531-88870908
Address:F Bldg,750#,Shunhua Rd,New&High-tech Zone,Jinan,Shandong,China 250101
Doi:10.1021/jo00020a003
(1991)Doi:10.1021/om201281w
(2012)Doi:10.1080/00397911.2010.542862
(2012)Doi:10.1002/chem.201102182
(2011)Doi:10.1002/chem.201102613
(2011)Doi:10.1021/jo00038a024
(1992)