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Letters in Drug Design & Discovery

Author(s): D. Zou, H.-X. Zhai, J. Eckman, P. Higgins, M. Gillard, L. Knerr, S. Carre, P. Pasau, P. Collart and J. Grassi

DOI: 10.2174/157018007780077381

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Novel, Acidic CCR2 Receptor Antagonists: From Hit to Lead

Page: [185 - 191] Pages: 7

  • * (Excluding Mailing and Handling)

Abstract

High throughput screening identified a pyrrolidinone containing acidic functionality as a CCR2 antagonist of modest affinity. We describe initial SAR around this hit, including solution phase parallel synthesis for analog preparation, and we describe identification and characterization of an analog subsequently selected as a viable lead molecule for further optimization.

Keywords: MCP-1, CCR2, Chemokine receptor, Antagonist, Inflammation, Hit to lead