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SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa by Jennifer X. Qiao; Chong-Hwan Chang; Daniel L. Cheney; Paul E. Morin; Gren Z. Wang; Sarah R. King; Tammy C. Wang; Alan R. Rendina; Joseph M. Luettgen; Robert M. Knabb; Ruth R. Wexler; Patrick Y.S. Lam is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa about?

In the search of Factor Xa (FXa) inhibitors structurally different from the pyrazole-based series, we identified a viable series of enantiopure cis-(1R,2S)-cycloalkyldiamine derivatives as potent and selective inhibitors of FXa. Among them, cyclohexyldiamide 7 and cyclopentyldiamide 9 were the most potent neutral compounds, and had good anticoagulant activity comparable to the pyrazole-based analogs. Crystal structures of 7-FXa and 9-FXa illustrate binding similarities and differences between the fiveand the six-membered core systems, and provide rationales for the observed SAR of P1 and linker moieties.

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Author

Jennifer X. Qiao; Chong-Hwan Chang; Daniel L. Cheney; Paul E. Morin; Gren Z. Wang; Sarah R. King; Tammy C. Wang; Alan R. Rendina; Joseph M. Luettgen; Robert M. Knabb; Ruth R. Wexler; Patrick Y.S. Lam

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)

Published

2007

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)