Enantiopure five-membered cyclicdiamine derivatives as potent and selective inhibitors of factor Xa. Improving in vitro metabolic stability via core modifications

JX Qiao, TC Wang, GZ Wang, DL Cheney, K He…

Index: Qiao, Jennifer X.; Wang, Tammy C.; Wang, Gren Z.; Cheney, Daniel L.; He, Kan; Rendina, Alan R.; Xin, Baomin; Luettgen, Joseph M.; Knabb, Robert M.; Wexler, Ruth R.; Lam, Patrick Y.S. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 18 p. 5041 - 5048

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Citation Number: 14

Abstract

We previously reported a series of enantiopure cis-(1R, 2S)-cyclopentyldiamine derivatives as potent and selective inhibitors of Factor Xa (FXa). Herein, we describe our approach to improve the metabolic stability of this series via core modifications. Multiple resulting series of compounds demonstrated similarly high FXa potency and improved metabolic stability in human liver microsomes compared with the cyclopentyldiamide 1.(3R, 4S)- ...