| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10591051 | Bioorganic & Medicinal Chemistry Letters | 2014 | 7 Pages |
Abstract
In an effort to identify a potential back-up to apixaban (Eliquis®), we explored a series of diversified P4 moieties. Several analogs with substituted gem-dimethyl moieties replacing the terminal lactam of apixaban were identified which demonstrated potent FXa binding affinity (FXa Ki), good human plasma anticoagulant activity (PT EC2x), cell permeability, and oral bioavailability.
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Authors
Michael J. Orwat, Jennifer X. Qiao, Kan He, Alan R. Rendina, Joseph M. Luettgen, Karen A. Rossi, Baomin Xin, Robert M. Knabb, Ruth R. Wexler, Patrick Y.S. Lam, Donald J.P. Pinto,