AI Article Synopsis
- The report discusses the creation of new CCR2 antagonists using unique non-aryl/heteroaryl RHS structures, challenging previous assumptions about necessary binding features.
- It presents structure-activity relationship (SAR) analysis focusing on three key factors: binding potency to the human CCR2 receptor, dofetilide activity, and metabolic stability in vitro.
- The study successfully identifies compounds with promising characteristics that can aid in exploring CCR2's role in various diseases.
Article Abstract
This report describes the design and synthesis of a series of CCR2 antagonists incorporating novel non-aryl/heteroaryl RHS (right hand side) motifs. Previous SAR in the area has suggested an aryl/heteroaryl substituent as a necessary structural feature for binding to the CCR2 receptor. Herein we describe the SAR with regards to potency (binding to hCCR2), dofetilide activity and metabolic stability (in vitro HLM) for this series. The resulting outcome was the identification of compounds with excellent properties for the investigation of the role of CCR2 in disease.
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| http://dx.doi.org/10.1016/j.bmcl.2011.01.052 | DOI Listing |
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