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Design and synthesis of novel CCR2 antagonists: investigation of non-aryl/heteroaryl binding motifs.

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Trujillo JI,Huang W,Hughes RO,Rogier DJ,Turner SR,Devraj R,Morton PA,Xue CB,Chao G,Covington MB,Newton RC,Metcalf B

doi

10.1016/j.bmcl.2011.01.052

subject

Has Abstract

pub_date

2011-03-15 00:00:00

pages

1827-31

issue

6

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)00075-8

journal_volume

21

pub_type

杂志文章

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