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Discovery of trisubstituted cyclohexanes as potent CC chemokine receptor 2 (CCR2) antagonists |
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| Authors: | Robert J Cherney John B Brogan Ruowei Mo Yvonne C Lo Gengjie Yang Persymphonie B Miller Peggy A Scherle Bruce F Molino Percy H Carter Carl P Decicco |
| Institution: | 1. Research and Development, Bristol-Myers Squibb Company, Princeton, NJ 08543-4000, USA;2. AMRI, 26 Corporate Circle, PO Box 15098, Albany, NY 12212, USA |
| 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 IC50 = 2.4 nM) and functional antagonism (calcium flux IC50 = 2.0 nM and chemotaxis IC50 = 5.1 nM). |
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