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Potent heteroarylpiperidine and carboxyphenylpiperidine 1-alkyl-cyclopentane carboxamide CCR2 antagonists

Pasternak, Alexander ; Goble, Stephen D. ; Vicario, Pasquale P. ; Di Salvo, Jerry ; Ayala, Julia M. ; Struthers, Mary ; Demartino, Julie A. ; Mills, Sander G. ; Yang, Lihu

Bioorganic & Medicinal Chemistry Letters, 2008, Vol.18(3), pp.994-998 [Peer Reviewed Journal]

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  • Title:
    Potent heteroarylpiperidine and carboxyphenylpiperidine 1-alkyl-cyclopentane carboxamide CCR2 antagonists
  • Author: Pasternak, Alexander ; Goble, Stephen D. ; Vicario, Pasquale P. ; Di Salvo, Jerry ; Ayala, Julia M. ; Struthers, Mary ; Demartino, Julie A. ; Mills, Sander G. ; Yang, Lihu
  • Description: This report describes incorporation of 4-heteroaryl piperidine and 4-(carboxyphenyl)-piperidine subunits into our CCR2 antagonists, leading to new analogs retaining CCR2 potency, but with improved selectivity over I Kr channel binding. This report describes replacement of the 4-(4-fluorophenyl)piperidine moiety in our CCR2 antagonists with 4-heteroaryl piperidine and 4-(carboxyphenyl)-piperidine subunits. Some of the resulting analogs retained potency in our CCR2 binding assay and had improved selectivity versus the I Kr channel; poor selectivity against I Kr had been a liability of earlier analogs in this series.
  • Is Part Of: Bioorganic & Medicinal Chemistry Letters, 2008, Vol.18(3), pp.994-998
  • Identifier: ISSN: 0960-894X ; DOI: 10.1016/j.bmcl.2007.12.029
  • Subjects: Ccr2 ; Antagonist ; Chemokine
  • Language: English

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