325464-63-9Relevant articles and documents
Development of potent and selective plasmin and plasma kallikrein inhibitors and studies on the structure-activity relationship
Okada, Yoshio,Tsuda, Yuko,Tada, Mayako,Wanaka, Keiko,Okamoto, Utako,Hijikata-Okunomiya, Akiko,Okamoto, Shosuke
, p. 1964 - 1972 (2007/10/03)
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.