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 MoreBeijing Apis Biotechnology Co., Ltd.
Contact:86-010-67856775-8551
Address:NO.4PUHUANGYU ROAD,FENTAI DISTRICT, BEIJING, CHINA
Contact:+86-579-85206992
Address:No 451 chouzhou north road ,room 1106 int'l business center , yiwu ,china
Shao Xing Empire Import&Export CO.,ltd
Contact:86-575-82127757
Address:11#, Weiwu Road, Shangyu Industrial Park, Hangzhou Bay, Hangzhou, Zhejiang Province, China
Contact:86+21-56421993
Address:3F,BUILDING 10,NO.2889 JINKE ROAD, SHANGHAI.
Shaanxi King Stone Enterprise Company Limited
Contact:86-29-88353805,13609285751
Address:.209 Keji Road Hi-Tech industrial Develpment Zone .Xian 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)
