Novel, Acidic CCR2 Receptor Antagonists: From Hit to Lead

D. Zou; H.-X. Zhai; J. Eckman; P. Higgins; M. Gillard; L. Knerr; S. Carre; P. Pasau; P. Collart; J. Grassi

doi:10.2174/157018007780077381

ISSN: 1570-1808
E-ISSN: 1875-628X

Novel, Acidic CCR2 Receptor Antagonists: From Hit to Lead
Authors: D. Zou¹, H.-X. Zhai², J. Eckman³, P. Higgins⁴, M. Gillard⁵, L. Knerr⁶, S. Carre⁷, P. Pasau⁸, P. Collart⁹ and J. Grassi¹⁰
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¹ Resolvyx Pharmaceuticals,Bedford, MA, USA. ² Resolvyx Pharmaceuticals,Bedford, MA, USA. ³ Resolvyx Pharmaceuticals,Bedford, MA, USA. ⁴ Resolvyx Pharmaceuticals,Bedford, MA, USA. ⁵ Resolvyx Pharmaceuticals,Bedford, MA, USA. ⁶ Resolvyx Pharmaceuticals,Bedford, MA, USA. ⁷ Resolvyx Pharmaceuticals,Bedford, MA, USA. ⁸ Resolvyx Pharmaceuticals,Bedford, MA, USA. ⁹ Resolvyx Pharmaceuticals,Bedford, MA, USA. ¹⁰ Resolvyx Pharmaceuticals,Bedford, MA, USA.
Source: Letters in Drug Design & Discovery, Volume 4, Issue 3, Apr 2007, p. 185 - 191
DOI: https://doi.org/10.2174/157018007780077381
- Available online: 01 Apr 2007

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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2007-04-01

2025-06-19

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Article Type: Research Article

Keyword(s): Antagonist; CCR2; Chemokine receptor; Hit to lead; Inflammation; MCP-1

Novel, Acidic CCR2 Receptor Antagonists: From Hit to Lead

Abstract

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