期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 11, 期 18, 页码 2475-2479出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(01)00492-9
关键词
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(2S)-2-(3-Chlorophenyl)-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-[spiro(2,3-dihydrobenzthiophene-3,4 ' -piperidin-1 ' -yl)]butane S-oxide (lb) 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-(benzyloxy-carbonyl)amino)piperidine derivatives (3-5) as potent CCR5 antagonists. (C) 2001 Elsevier Science Ltd. All rights reserved.
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