Title of article :
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 1: discovery of the pyrrolidine scaffold and determination of its stereochemical requirements
Author/Authors :
Jeffrey J. Hale، نويسنده , , Richard J. Budhu، نويسنده , , Sander G. Mills، نويسنده , , Malcolm MacCoss، نويسنده , , Lorraine Malkowitz، نويسنده , , Salvatore Siciliano، نويسنده , , Sandra L. Gould، نويسنده , , Julie A. DeMartino، نويسنده , , Martin S. Springer، نويسنده ,
Abstract :
A series of 1,3,4-trisubstituted pyrrolidines was discovered to have the ability to displace [125I]-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.
