Bioorganic & medicinal chemistry

Conformationally restricted analogs of the direct thrombin inhibitor FM 19

EA Girnys, VR Porter, HI Mosberg

Index: Girnys, Elizabeth A.; Porter, Vanessa R.; Mosberg, Henry I. Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 24 p. 7425 - 7434

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Citation Number: 5

Abstract

The serine protease thrombin plays several key roles in the clotting cascade within the hemostatic system, such as in fibrin formation and platelet activation. Thus, development of an inhibitor that binds to the enzyme's active site (a direct thrombin inhibitor) offers an approach for the treatment of thrombus-associated diseases. Previous structure–activity relationship studies originally based on the bradykinin breakdown product Arg-Pro-Pro- ...