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

ID: ALA1134084

Journal: Bioorg Med Chem Lett

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

Authors: Hale JJ, Budhu RJ, Mills SG, MacCoss M, Malkowitz L, Siciliano S, Gould SL, DeMartino JA, Springer MS.

Abstract: A series of 1,3,4-trisubstituted pyrrolidines was discovered to have the ability to displace [(125)I]-MIP-1alpha 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.

CiteXplore: 11378372

DOI: 10.1016/s0960-894x(01)00232-3

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