期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 16, 期 19, 页码 8875-8881出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.08.061
关键词
dopamine receptor; conformational restriction; cyclopropane
资金
- Japan Society for the Promotion of Science
A series of the cyclopropane-based conformationally restricted analogs of haloperidol were designed as potential antidopaminergic agents and were effectively synthesized using highly stereoselective Grignard reaction with tert-butanesulfinyl imines as the key step. Pharmacological evaluation of the compounds showed that the conformational restriction method can effectively work for improving the pharmacological selectivity of a parent compound and also for investigating the bioactive conformation. (C) 2008 Elsevier Ltd. All rights reserved.
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