Journal of Medicinal Chemistry p. 285 - 289 (1981)
Update date:2022-07-30
Topics:
Falch, Erik
Krogsgaard-Larsen, Povl
The syntheses of the methyl ester, butyl ester, (ethoxycarbonyl)methyl ester, and 11 (acyloxy)methyl esters of the potent γ-aminobutyric acid agonist isoguvacine (1,2,3,6-tetrahydropyridine-4-carboxylic acid) are described.The chemical stability of the esters and their in vitro rates of hydrolysis under approximately physiological conditions by nonspecific esterases from human serum were examined.A selected number of the esters were tested for antagonism of convulsions induced by bicuculline, isoniazide, and by electroshock.While the compounds showed only weak activities in the bicuculline and isoniazide tests, a good correlation between in vitro rates of enzymatic hydrolysis and the time of onset of the antagonism of the electroshock-induced convulsions could be found.
View MoreSHAANXI FUJIE PHARMACEUTICAL CO.,LTD
website:http://www.fujiepharm.com
Contact:+86-29-63650906
Address:Yuanqu Yi Road, Qinghe Food Industrial Park, Sanyuan County, Shaanxi Province, China
Chemsigma International Co.,Ltd.
website:http://www.chemsigma.com
Contact:86-025-58748998
Address:Rm.705, 15th Building,Rd.Xinke II
Contact:86-574-26865651
Address:529 YuanBaoShan Road, Beilun District
Shandong Ailitong New Material Co.,Ltd
Contact:+86-536-3226266
Address:zhongjia village, putong town , qingzhou city,Shandong Province,China
Jurong Huaheng Natural Biological Products Factory
website:http://www.risebiochem.com
Contact:+86-13921007726
Address:Chuncheng town,Jurong city,Jiangsu province,China
Doi:10.1021/ja01105a037
(1953)Doi:10.1039/P29790000423
(1979)Doi:10.1021/jo01099a024
(1958)Doi:10.1021/acs.organomet.5b00385
(2015)Doi:10.1016/S0022-328X(00)98691-1
(1984)Doi:10.1016/j.bmcl.2009.10.045
(2009)