Bioorganic and Medicinal Chemistry Letters, volume 21, issue 6, pages 1827-1831

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

JOHN L. TRUJILLO 1
Wei Huang 1
Robert O Hughes 1
D Joseph Rogier 1
Steven R Turner 1
Rajesh Devraj 1
Philip A. Morton 2
Chu-Biao Xue 3
Ganfeng Chao 3
Maryanne B. Covington 4
Robert Newton 4
Brian Metcalf 3
Show full list: 12 authors
1
 
Department of Medicinal Chemistry, Pfizer Global Research and Development, Chesterfield, MO 63017, USA
2
 
Department of Biochemical Pharmacology, Pfizer Global Research and Development, Chesterfield, MO 63017, USA
3
 
Department of Medicinal Chemistry, Incyte Corporation, Wilmington, DE, USA
4
 
Department of Biochemstry/Enzymology, Incyte Corporation, Wilmington, DE, USA
Publication typeJournal Article
Publication date2011-03-01
scimago Q2
wos Q2
SJR0.508
CiteScore5.7
Impact factor2.5
ISSN0960894X, 14643405
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
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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