Literature DB >> 17482462

3-Amino-1-alkyl-cyclopentane carboxamides as small molecule antagonists of the human and murine CC chemokine receptor 2.

Gabor Butora1, Richard Jiao, William H Parsons, Pasquale P Vicario, Hong Jin, Julia M Ayala, Margaret A Cascieri, Lihu Yang.   

Abstract

A series of low molecular weight antagonists of both the human and murine CC chemokine receptor 2, containing a 1-alkyl-3-(3-methyl-4-spiroindenylpiperidine)-substituted cyclopentanecarboxamide, is described. A SAR study of the C(1) substituent revealed that short, branched alkyl groups such as isopropyl, isobutyl, or cyclopropyl are optimal for both human and murine CCR2 binding activity.

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Year:  2007        PMID: 17482462     DOI: 10.1016/j.bmcl.2007.04.053

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Binding site characterization of G protein-coupled receptor by alanine-scanning mutagenesis using molecular dynamics and binding free energy approach: application to C-C chemokine receptor-2 (CCR2).

Authors:  Swapnil Chavan; Shirishkumar Pawar; Rajesh Singh; M Elizabeth Sobhia
Journal:  Mol Divers       Date:  2012-04-22       Impact factor: 2.943

  1 in total

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