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

Structure-activity relationship studies directed toward the optimization of (2S)-2-(3-chlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[-(substituted)piperidin-1-yl]butanes as CCR5 antagonists resulted in the synthesis of the spiro-indanone derivative 8c (IC50 = 5 nM). These and previous results are summarized in a proposed pharmacophore model for this class of CCR5 antagonist. (C) 2001 Elsevier Science Ltd. All rights reserved.