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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(1971)
