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
Citation
Jj. Hale et al., 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 1: Discovery of the pyrrolidine scaffold and determination of its stereochemical requirements, BIOORG MED, 11(11), 2001, pp. 1437-1440
Citations number
24
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
11
Year of publication
2001
Pages
1437 - 1440
Database
ISI
SICI code
0960-894X(20010604)11:11<1437:1PCRAP>2.0.ZU;2-2
Abstract
A series of 1,3,4-trisubstituted pyrrolidines was discovered to have the ab ility to displace [I-125]-MIP-1 alpha from the CCR5 receptor expressed on C hinese hamster ovary (CHO) cell membranes. CCR5 activity was found to be de pendent on the regiochemistry and the absolute stereochemistry of the pyrro lidine. (C) 2001 Elsevier Science Ltd. All rights reserved.