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
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2001 Jun 04; Vol. 11 (11), pp. 1437-40.
Publication Year :: 2001
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.

Subjects :: Animals
Binding, Competitive
CHO Cells
Chemokine CCL4
Cricetinae
Iodine Radioisotopes
Macrophage Inflammatory Proteins chemistry
Macrophage Inflammatory Proteins pharmacology
Molecular Conformation
Pyrrolidines chemistry
Receptors, CCR5 genetics
Transfection
CCR5 Receptor Antagonists
Pyrrolidines pharmacology

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