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
Letters in Drug Design & Discovery
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.
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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
DOI https://dx.doi.org/10.2174/157018007780077381 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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