Development of potent and selective plasmin and plasma kallikrein inhibitors and studies on the structure-activity relationship

DOI: 10.1248/cpb.48.1964

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Chemical and Pharmaceutical Bulletin p. 1964 - 1972 (2000)

Update date:2022-07-29

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Authors:

Okada, Yoshio

Tsuda, Yuko

Tada, Mayako

Wanaka, Keiko

Okamoto, Utako

Hijikata-Okunomiya, Akiko

Okamoto, Shosuke

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Article abstract of DOI:10.1248/cpb.48.1964

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.

Full text of DOI:10.1248/cpb.48.1964

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