Novel, Acidic CCR2 Receptor Antagonists: Lead Optimization

Title: Novel, Acidic CCR2 Receptor Antagonists: Lead Optimization

Volume: 4 Issue: 4

Author(s): O. A. Dasse, J. L. Evans, H.-X. Zhai, D. Zou, J. T. Kintigh, F. Chan, K. Hamilton, E. Hill, J. B. Eckman, P. J. Higgins, A. Volosov, P. Collart, J.-M. Nicolas, R.K. Kondru and C.E. Schwartz

Affiliation:

Keywords: MCP-1, CCR2, Chemokine receptor, Antagonist, Medicinal chemistry, Lead optimization, CoMFA, Pharmacophore

Abstract: A unique pyrrolidinone-based CCR2 antagonist with sub-micromolar in vitro activities, good selectivity, and reasonable ADME properties was identified following a screening campaign and subsequent hit-to-lead medicinal chemistry efforts. We now describe further modification of this lead molecule to provide compounds with excellent DMPK profiles and significantly enhanced in vitro activities.

Cite this article as:

Dasse A. O., Evans L. J., Zhai H.-X., Zou D., Kintigh T. J., Chan F., Hamilton K., Hill E., Eckman B. J., Higgins J. P., Volosov A., Collart P., Nicolas J.-M., Kondru R.K. and Schwartz C.E., Novel, Acidic CCR2 Receptor Antagonists: Lead Optimization, Letters in Drug Design & Discovery 2007; 4 (4) . https://dx.doi.org/10.2174/157018007784619989

DOI https://dx.doi.org/10.2174/157018007784619989	Print ISSN 1570-1808
Publisher Name Bentham Science Publisher	Online ISSN 1875-628X