Chemokines are endogenous proteins that are involved in the migration of leukocytes to points of inflammation.  We have been interested in the chemokine, monocyte chemoattractant protein-1 (MCP-1 or CCL2), as it is overexpressed in many autoimmune and inflammatory conditions.  MCP-1 induces its functional response via its cell surface-expressed receptor, CC chemokine receptor 2 (CCR2), which is a G protein-coupled receptor.  It is thought that antagonism of this pair (CCR2/MCP-1) could hold promise as a potential therapeutic for a host of diseases, including rheumatoid arthritis, atherosclerosis, multiple sclerosis, and diabetes.  In this disclosure, we describe novel, potent, and bioavailable trisubstituted cyclohexane derivatives as CCR2 antagonists.

Discovery of novel trisubstituted cyclohexane derivatives as potent and bioavailable CCR2 antagonists

245th National Meeting (2013)

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