| Literature DB >> 24951330 |
Michael J Orwat1, Jennifer X Qiao2, Kan He2, Alan R Rendina2, Joseph M Luettgen2, Karen A Rossi2, Baomin Xin2, Robert M Knabb2, Ruth R Wexler2, Patrick Y S Lam2, Donald J P Pinto2.
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.Entities:
Keywords: Factor Xa inhibitors; Thromboembolic disorders
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Year: 2014 PMID： 24951330 DOI： 10.1016/j.bmcl.2014.05.101
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823