| Literature DB >> 25592713 |
James R Corte1, Tianan Fang2, Jon J Hangeland2, Todd J Friends2, Alan R Rendina2, Joseph M Luettgen2, Jeffrey M Bozarth2, Frank A Barbera2, Karen A Rossi2, Anzhi Wei2, Vidhyashankar Ramamurthy2, Paul E Morin2, Dietmar A Seiffert2, Ruth R Wexler2, Mimi L Quan2.
Abstract
The structure-activity relationships (SAR) of six-membered ring replacements for the imidazole ring scaffold is described. This work led to the discovery of the potent and selective pyridine (S)-23 and pyridinone (±)-24 factor XIa inhibitors. SAR and X-ray crystal structure data highlight the key differences between imidazole and six-membered ring analogs.Entities:
Keywords: Activated partial thromboplastin time; FXIa; Factor XIa inhibitors; Thrombosis; aPTT
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Year: 2014 PMID： 25592713 DOI： 10.1016/j.bmcl.2014.12.050
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823