期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 17, 期 14, 页码 5015-5026出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.05.064
关键词
NPY; Neuropeptide Y; Y5 receptor; Spiroindoline; Obesity; Phenyl imidazole
Spiroindoline urea derivatives, designed to act as NPY Y5 receptor antagonists, were synthesized and their structure-activity relationships were investigated. Of these derivatives, compound 3a showed good Y5 binding affinity with favorable pharmacokinetic properties. Compound 3a significantly inhibited bPP Y5 agonist-induced food intake in rats, and suppressed body weight gain in DIO mice. (C) 2009 Elsevier Ltd. All rights reserved.
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