Development of plasmin-selective inhibitors and studies of their structure-activity relationship

Authors
Okada, Y Matsumoto, Y Tsuda, Y Tada, M Wanaka, K Hijikata-Okunomiya, A Okamoto, S
Citation
Y. Okada et al., Development of plasmin-selective inhibitors and studies of their structure-activity relationship, CHEM PHARM, 48(2), 2000, pp. 184-193
Citations number
19
Categorie Soggetti
Chemistry & Analysis
Journal title
CHEMICAL & PHARMACEUTICAL BULLETIN
ISSN journal
00092363 → ACNP
Volume
48
Issue
2
Year of publication
2000
Pages
184 - 193
Database
ISI
SICI code
0009-2363(200002)48:2<184:DOPIAS>2.0.ZU;2-O
Abstract
Various compounds were synthesized by combining three components at positio ns P1, P-1' and P-2'. Of these, N-(trans-4-aminomethylcyclohexanecarbonyl)- Tyr(O-2-bromobenzyloxycarbonyl)-octylamide inhibited plasmin selectively wi th IC50 values of 0.80 and 0.23 mu M towards S-2251 and fibrin, respectivel y This compound also inhibited plasma kallikrein, urokinase, thrombin and t rypsin with IC50 values of 10, >50, >50 and 1.6 mu M, respectively.