Design and Synthesis of Isoxazoline Derivatives as Factor Xa Inhibitors. 1 1

…, CD Ellis, JR Pruitt, DJ Carini, LL Bostrom…

Index: Quan, Mimi L.; Liauw, Ann Y.; Ellis, Christopher D.; Pruitt, James R.; Carini, David J.; Bostrom, Lori L.; Huang, Peggy P.; Harrison, Kimberly; Knabb, Robert M.; Thoolen, Martin J.; Wong, Pancras C.; Wexler, Ruth R. Journal of Medicinal Chemistry, 1999 , vol. 42, # 15 p. 2752 - 2759

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Citation Number: 76

Abstract

Thrombosis is a major cause of mortality in the industrialized world. Therefore, the prevention of blood coagulation has become a major target for new therapeutic agents. One attractive approach is the inhibition of factor Xa (FXa), the enzyme directly responsible for prothrombin activation. We report a series of novel biaryl-substituted isoxazoline derivatives in which the biaryl moiety was designed to interact with the S4 aryl-binding domain of the ...