Chemical and Pharmaceutical Bulletin p. 1964 - 1972 (2000)
Update date:2022-07-29
Topics:
Okada, Yoshio
Tsuda, Yuko
Tada, Mayako
Wanaka, Keiko
Okamoto, Utako
Hijikata-Okunomiya, Akiko
Okamoto, Shosuke
Based on structure-activity relationship studies, we designed and synthesized plasmin (PL) and plasma kallikrein (PK) inhibitors. Trans-(4-aminomethylcyclohexanecarbonyl)-Tyr(O-PIC)-octylamide inhibited PL, PK, urokinase (UK) and thrombin (TH) with IC50 values of 0.53, 30, 5.3 and >400 μM, respectively. Trans-(4-aminomethylcyclohexanecarbonyl)-Tyr(O-2-Pyrim)-4-carboxyanilide inhibited PL, PK, UK and TH with IC50 values of 36, 0.56, 440 and >1000 μM, respectively.
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Doi:10.1016/j.jorganchem.2014.06.018
(2014)Doi:10.1039/c9cc06638a
(2019)Doi:10.1016/j.bmcl.2007.04.089
(2007)Doi:10.1021/acs.joc.9b03155
(2020)Doi:10.1039/b007626k
(2000)Doi:10.1016/S0040-4020(01)98216-X
(1971)
