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ID: ALA2016523

Journal: Bioorg Med Chem Lett

Title: Discovery of an orally-bioavailable CC Chemokine Receptor 2 antagonist derived from an acyclic diaminoalcohol backbone.

Authors: Carter PH, Brown GD, King SR, Voss ME, Tebben AJ, Cherney RJ, Mandlekar S, Lo YC, Yang G, Miller PB, Scherle PA, Zhao Q, Decicco CP.

Abstract: We describe an isostere-driven approach to improve upon a previously-described series of capped dipeptide antagonists of CC Chemokine Receptor 2 (CCR2). Modification of the substitution around the isostere was combined with additional changes in a distal aromatic substituent to provide single-digit nanomolar antagonists of CCR2. These studies led to the identification of 18, a compound that was suitable for studies in murine models of CCR2 activity.

CiteXplore: 22475558

DOI: 10.1016/j.bmcl.2012.03.007