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 MoreSHANDONG QINGYUNCHANGXIN CHEMICAL SCIENCE-TECH CO.,LTD
Contact:86-21-60560171
Address:1689Donghuan Rade,Qingyun County, Dezhou City, Shandong,China
Wuhan Chemwish Technology Co., Ltd
website:http://www.chemwish.com/
Contact:+86-27-67849912
Address:Room 1311, Unit 2, Block1, Innovation Road East Lake High-tech Development Zone Wuhan, Hubei，P.R. China
Contact:0027-717-456976
Address:2ND FLOOR, 325 VAUSE ROAD, OVERPORT, 4001, SOUTH AFRICA
Contact:86-511-85210668 0511-85210668, 85210818, 85210898
Address:Yihai Garden E-902,NO.99 Daxi RD., Zhenjiang Jiiangsu ,China
CHANGYI CITY FENGRUN FINE CHEMICAL CO.,LTD
website:http://www.fengrunhuagong.com
Contact:+86-536-7869976
Address:Changyi Coastal Economic Development Zone
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)
