Chemical and Pharmaceutical Bulletin p. 1079 - 1090 (1993)
Update date:2022-08-04
Topics:
Teno
Wanaka
Okada
Taguchi
Okamoto
Hijikata-Okunomiya
Okamoto
The molecule of trans-4-aminomethylcyclohexanecarbonylphenylalanine 4- carboxymethylanilide (8), which is a potent and selective inhibitor of plasma kallikrein, can be divided into three parts (P1, P1 and P2), each of which contains one of the rings. In order to study the role of each part in the manifestation of potent and selective inhibitory activity and the relationship between the structure and inhibitory activities toward plasmin, plasma kallikrein, urokinase and thrombin, each part was substituted with various other moieties to give many kinds of analogs and their inhibitory activities against the above enzymes were examined. Among them, trans-4- aminomethylcyclohexanecarbonyl-O-2-bromobenzyloxycarbonyltyrosine 4- acetylanilide (12) inhibited plasmin and plasma kallikrein with IC50 values of 2.3 x 10-7 M and 3.7 x 10-7 M, and K(i) values of 1.2 x 10-7 M and 1.3 x 10-7 M, respectively.
View MoreJiangxi Dongxu Chemical Science & Technology Co.,Ltd
Contact:+86-791-86899381
Address:Nanchang, Jiangxi, China
ShiJiaZhuang Dowell Chemical Co.,Ltd.
website:http://www.dowechem.com
Contact:+86-13463963265
Address:Xiyangling village, high tech Zone, Shijiazhuang，Hebei, China
Contact:+86-10-67147360/67107388
Address:No.18 Guangming Zhongjie, Chongwen District, Beijing, 100061, China
Suzhou Sinosun Imp.&Exp. Corporation
website:http://www.szsinosun.com
Contact:+86-512-63488895,63488616
Address:No.758 East Jiangling Road Wujiang Economic & Technological Developmenty Zone Jiangsu China
SHANDONG CREDAGRI CHEMICAL CO., LTD.
Contact:+86-531-88872050
Address:ROOM 601A, BUILDING 2, SHUNTAI SQUARE, NO. 2000 SHUNHUA ROAD, HI-TECH DEVELOPMENT ZONE, JINAN, CHINA.
Doi:10.1021/jacs.9b06739
(2019)Doi:10.1021/jo00076a070
(1993)Doi:10.1248/cpb.48.108
(2000)Doi:10.1016/S0022-1139(00)80093-7
(1993)Doi:10.1016/j.bmcl.2014.11.047
(2015)Doi:10.1016/j.bmc.2013.11.029
(2014)
