| Literature DB >> 11549450 |
P E Finke1, B Oates, S G Mills, M MacCoss, L Malkowitz, M S Springer, S L Gould, J A DeMartino, A Carella, G Carver, K Holmes, R Danzeisen, D Hazuda, J Kessler, J Lineberger, M Miller, W A Schleif, E A Emini.
Abstract
(2S)-2-(3-Chlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[spiro(2,3-dihydrobenzthiophene-3,4'-piperidin-1'-yl)]butane S-oxide (1b) has been identified as a potent CCR5 antagonist having an IC50=10 nM. Herein, structure-activity relationship studies of non-spiro piperidines are described, which led to the discovery of 4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidine derivatives (3-5) as potent CCR5 antagonists.Entities:
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Year: 2001 PMID： 11549450 DOI： 10.1016/s0960-894x(01)00492-9
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823