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  • Title: Structure-activity relationships of the oxindole growth hormone secretagogues.
    Author: Tokunaga T, Hume WE, Nagamine J, Kawamura T, Taiji M, Nagata R.
    Journal: Bioorg Med Chem Lett; 2005 Apr 01; 15(7):1789-92. PubMed ID: 15780607.
    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.
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