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1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 1: discovery of the pyrrolidine scaffold and determination of its stereochemical requirements

Hale, Jeffrey J. ; Budhu, Richard J. ; Mills, Sander G. ; Maccoss, Malcolm ; Malkowitz, Lorraine ; Siciliano, Salvatore ; Gould, Sandra L. ; Demartino, Julie A. ; Springer, Martin S.

Bioorganic & Medicinal Chemistry Letters, 2001, Vol.11(11), pp.1437-1440 [Peer Reviewed Journal]

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  • Title:
    1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 1: discovery of the pyrrolidine scaffold and determination of its stereochemical requirements
  • Author: Hale, Jeffrey J. ; Budhu, Richard J. ; Mills, Sander G. ; Maccoss, Malcolm ; Malkowitz, Lorraine ; Siciliano, Salvatore ; Gould, Sandra L. ; Demartino, Julie A. ; Springer, Martin S.
  • Description: A series of 1,3,4-trisubstituted pyrrolidines was discovered to have the ability to displace [ 125 I]-MIP-1α from the CCR5 receptor expressed on Chinese hamster ovary (CHO) cell membranes. CCR5 activity was found to be dependent on the regiochemistry and the absolute stereochemistry of the pyrrolidine. A series of 1,3,4-trisubstituted pyrrolidines was discovered to have the ability to displace [ 125 I]-MIP-1α from the CCR5 receptor expressed on Chinese hamster ovary (CHO) cell membranes. CCR5 activity was found to be dependent on the regiochemistry and the absolute stereochemistry of the pyrrolidine.
  • Is Part Of: Bioorganic & Medicinal Chemistry Letters, 2001, Vol.11(11), pp.1437-1440
  • Identifier: ISSN: 0960-894X ; DOI: 10.1016/S0960-894X(01)00232-3
  • Subjects: Ccr5 Receptor Antagonists ; Pyrrolidines -- Pharmacology
  • Language: English

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