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Bioorg Med Chem Lett. 2005 Apr 1;15(7):1789-92.

Structure-activity relationships of the oxindole growth hormone secretagogues.

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1
Research Division, Sumitomo Pharmaceuticals Co., Ltd, 1-98 Kasugade Naka 3-chome, Konohana-ku, Osaka 554-0022, Japan.

Abstract

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 (IC(50)=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.

PMID:
15780607
DOI:
10.1016/j.bmcl.2005.02.042
[Indexed for MEDLINE]
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