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 Province Bethel Pharmaceutical Co., Ltd.
Contact:+86-795-259 3456 ，+86-15957688008 13566650571
Address:Huangjindui Chemical Park， Shanggao County ，Yichun city，Jiangxi Province
Shenyang Mole pharmaceutical Technology Development Co.,Ltd
Contact:+86-24-31204918/13889278616
Address:No.44, wanliutang road, shenhe District of Shenyang
Jiangsu Chiatai Qingjiang Pharmaceutical Co.,Ltd
Contact:+86-517-86283327
Address:9 North Hantai Road, Huaian, China
website:http://www.shtopchem.com/
Contact:0086-0576-87776998
Address:room no 1608,xuhui business building yude road,xujiahui street, xuhui district
Lyrin Industrial Corporation Limited
Contact:86-731-82571800
Address:Rm 2408,Asia Economy International Building,Shaoshan Road South,Yuhua District,Changsha,Hunan,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)
