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Conformational studies of 3-amino-1-alkyl-cyclopentane carboxamide CCR2 antagonists leading to new spirocyclic antagonists

Pasternak, Alexander ; Goble, Stephen D. ; Doss, George A. ; Tsou, Nancy N. ; Butora, Gabor ; Vicario, Pasquale P. ; Ayala, Julia Marie ; Struthers, Mary ; Demartino, Julie A. ; Mills, Sander G. ; Yang, Lihu

Bioorganic & Medicinal Chemistry Letters, 2008, Vol.18(4), pp.1374-1377 [Peer Reviewed Journal]

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  • Title:
    Conformational studies of 3-amino-1-alkyl-cyclopentane carboxamide CCR2 antagonists leading to new spirocyclic antagonists
  • Author: Pasternak, Alexander ; Goble, Stephen D. ; Doss, George A. ; Tsou, Nancy N. ; Butora, Gabor ; Vicario, Pasquale P. ; Ayala, Julia Marie ; Struthers, Mary ; Demartino, Julie A. ; Mills, Sander G. ; Yang, Lihu
  • Description: Evaluation of CCR2 binding affinities of conformationally constrained CCR2 antagonist analogs gave insight into the optimal relative positions of the piperidine and benzylamide moieties while simultaneously leading to the discovery of a new, potent lead type based upon a spirocyclic acetal scaffold. In an effort to shed light on the active binding conformation of our 3-amino-1-alkyl-cyclopentane carboxamide CCR2 antagonists, we prepared several conformationally constrained analogs resulting from backbone cyclization. Evaluation of CCR2 binding affinities for these analogs gave insight into the optimal relative positions of the piperidine and benzylamide moieties while simultaneously leading to the discovery of a new, potent lead type based upon a spirocyclic acetal scaffold.
  • Is Part Of: Bioorganic & Medicinal Chemistry Letters, 2008, Vol.18(4), pp.1374-1377
  • Identifier: ISSN: 0960-894X ; DOI: 10.1016/j.bmcl.2008.01.016
  • Subjects: Ccr2 ; Chemokine ; Antagonist
  • Language: English

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