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- ISSN: 1570-1808
- E-ISSN: 1875-628X
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Novel, Acidic CCR2 Receptor Antagonists: Lead Optimization
- Source: Letters in Drug Design & Discovery, Volume 4, Issue 4, Jun 2007, p. 263 - 271
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- 01 Jun 2007
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.
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