Biaryl substituted alkylboronate esters as thrombin inhibitors

…, J Wityak, C Dominguez, JV Duncia, CA Kettner…

Index: Quan; Wityak; Dominguez; Duncia; Kettner; Ellis; Liauw; Park; Santella; Knabb; Thoolen; Weber; Wexler Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 13 p. 1595 - 1600

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Citation Number: 20

Abstract

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 ...