Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 3: A proposed pharmacophore model for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)4-[4-(substituted)piperidin-1yl]butanes

Authors
Finke, PE Meurer, LC Oates, B Shah, SK Loebach, JL Mills, SG MacCoss, M Castonguay, L Malkowitz, L Springer, MS Gould, SL DeMartino, JA
Citation
Pe. Finke et al., Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 3: A proposed pharmacophore model for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)4-[4-(substituted)piperidin-1yl]butanes, BIOORG MED, 11(18), 2001, pp. 2469-2473
Citations number
20
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
18
Year of publication
2001
Pages
2469 - 2473
Database
ISI
SICI code
0960-894X(20010917)11:18<2469:AOTHCR>2.0.ZU;2-L
Abstract
Structure-activity relationship studies directed toward the optimization of (2S)-2-(3-chlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[-(substi tuted)piperidin-1-yl]butanes as CCR5 antagonists resulted in the synthesis of the spiro-indanone derivative 8c (IC50 = 5 nM). These and previous resul ts are summarized in a proposed pharmacophore model for this class of CCR5 antagonist. (C) 2001 Elsevier Science Ltd. All rights reserved.