Novel, Acidic CCR2 Receptor Antagonists: From Hit to Lead

Title: Novel, Acidic CCR2 Receptor Antagonists: From Hit to Lead

Volume: 4 Issue: 3

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

Affiliation:

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

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.

Cite this article as:

Zou D., Zhai H.-X., Eckman J., Higgins P., Gillard M., Knerr L., Carre S., Pasau P., Collart P. and Grassi J., Novel, Acidic CCR2 Receptor Antagonists: From Hit to Lead, Letters in Drug Design & Discovery 2007; 4 (3) . https://dx.doi.org/10.2174/157018007780077381