Bioorganic and Medicinal Chemistry Letters p. 1595 - 1600 (1997)
Update date:2022-08-04
Topics:
Quan
Wityak
Dominguez
Duncia
Kettner
Ellis
Liauw
Park
Santella
Knabb
Thoolen
Weber
Wexler
Thrombin is a serine protease that plays an important role in the blood coagulation cascade, and is a target enzyme for new therapeutic agents. Ac- (D)-Phe-Pro-boroArg-OH (DuP 714) was found to be a highly effective thrombin inhibitor. In order to reduce the peptidic nature of DuP 714, we have designed a series of novel biaryl substituted alkylboronate esters as potent thrombin inhibitors. The most potent compounds have subnanomolar affinity for thrombin.
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