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Bioorg Med Chem Lett. 2009 Feb 1;19(3):597-601. doi: 10.1016/j.bmcl.2008.12.062. Epub 2008 Dec 24.

Discovery of trisubstituted cyclohexanes as potent CC chemokine receptor 2 (CCR2) antagonists.

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1
Research and Development, Bristol-Myers Squibb Company, Princeton, NJ 08543-4000, USA. robert.cherney@bms.com

Abstract

A series of trisubstituted cyclohexanes was designed, synthesized and evaluated as CC chemokine receptor 2 (CCR2) antagonists. This led to the identification of two distinct substitution patterns about the cyclohexane ring as potent and selective CCR2 antagonists. Compound 36 exhibited excellent binding (CCR2 IC(50)=2.4 nM) and functional antagonism (calcium flux IC(50)=2.0 nM and chemotaxis IC(50)=5.1 nM).

PMID:
19131247
DOI:
10.1016/j.bmcl.2008.12.062
[Indexed for MEDLINE]
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