期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 21, 页码 5964-5968出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.07.065
关键词
CCR2 antagonist; MCP-1
A series of phenyl piperidine derivatives possessing potent and selective CCR2 antagonist activity is reported. Structure activity relationship (SAR) studies have established that incorporation of a second ring system adjacent to the aryl piperidine plays an important role in determining the CCR2 potency. Both a second piperidine ring and a 1,3-substituted cyclopentylamine have been probed as linkers. For the cyclopentylamine series, the IS,3R-configuration exhibits much higher affinity for hCCR2 than the 1R,3S-configuration. Compound 3g shows good selectivity over CCR 1, CCR3, 5-HT and has an excellent P450 profile. (c) 2007 Elsevier Ltd. All rights reserved.
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