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Bioorg Med Chem Lett. 2015 Feb 15;25(4):925-30. doi: 10.1016/j.bmcl.2014.12.050. Epub 2014 Dec 31.

Pyridine and pyridinone-based factor XIa inhibitors.

Author information

1
Discovery Chemistry and Cardiovascular Biology, Research and Development, Bristol-Myers Squibb Company, 311 Pennington-Rocky Hill Road, Pennington, NJ 08543, United States. Electronic address: james.corte@bms.com.
2
Discovery Chemistry and Cardiovascular Biology, Research and Development, Bristol-Myers Squibb Company, 311 Pennington-Rocky Hill Road, Pennington, NJ 08543, United States.

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.

KEYWORDS:

Activated partial thromboplastin time; FXIa; Factor XIa inhibitors; Thrombosis; aPTT

PMID:
25592713
DOI:
10.1016/j.bmcl.2014.12.050
[Indexed for MEDLINE]

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