Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infection

Authors
Kim, D Wang, LP Caldwell, CG Chen, P Finke, PE Oates, B MacCoss, M Mills, SG Malkowitz, L Gould, SL DeMartino, JA Springer, MS Hazuda, D Miller, M Kessler, J Danzeisen, R Carver, G Carella, A Holmes, K Lineberger, J Schleif, WA Emini, EA
Citation
D. Kim et al., Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infection, BIOORG MED, 11(24), 2001, pp. 3103-3106
Citations number
11
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
24
Year of publication
2001
Pages
3103 - 3106
Database
ISI
SICI code
0960-894X(200112)11:24<3103:DSASOH>2.0.ZU;2-D
Abstract
Replacement of the large hydantoin-indole moiety from our previous work wit h a variety of smaller heterocyclic analogues gave rise to potent CCR5 anta gonists having binding affinity comparable to the hydantoin analogues, The synthesis, SAR, and biological profiles of this class of antagonists are de scribed. (C) 2001 Elsevier Science Ltd. All rights reserved.