期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 7, 页码 2385-2389出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.02.061
关键词
rimonabant; anti-obesity; cannabinoid receptor antagonist; tetrazolerimonabant; anti-obesity; cannabinoid receptor antagonist; tetrazole
Cannabinoid CB1 receptors have been the focus of extensive studies since the first clinical results of rimonabant (SR141716) for the treatment of obesity and related metabolic disorders were reported in 2001. To further evaluate the properties of CB receptors, we have designed a new series of tetrazole-biarylpyrazoles. The various analogues were efficiently prepared and bioassayed for binding to cannabinoid CB1 receptor. Six of the new compounds which displayed high in vitro CB1 binding affinities were assayed for binding to CB2 receptor. Noticeably, cyclopentyl-tetrazole (9a) demonstrated good binding affinity and selectivity for CB1 receptor (IC50 = 11.6 nM and CB2/CB1 = 366). (C) 2008 Elsevier Ltd. All rights reserved.
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