期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 15, 期 7, 页码 1789-1792出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.02.042
关键词
ghrelin; growth hormone secretagogue; SM-130686
A series of substituted oxindole derivatives of SM-130686 was synthesized and evaluated as ghrelin receptor agonists. Modification of the substituents on the C3-aromatic part of the oxindole led to compounds with subnanomolar binding affinities. Compound 4i (IC50 = 0.02 nM) was orally active at low doses and showed in vivo activity when orally administered, 2 mg/kg twice a day for 4 days, as evidenced by significant body weight gain. (c) 2005 Elsevier Ltd. All rights reserved.
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