Oxindole derivatives as orally active potent growth hormone secretagogues

…, K Okazaki, Y Ueki, K Kumagai, S Hourai…

Index: Tokunaga; Hume; Umezome; Okazaki; Ueki; Kumagai; Hourai; Nagamine; Seki; Taiji; Noguchi; Nagata Journal of Medicinal Chemistry, 2001 , vol. 44, # 26 p. 4641 - 4649

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Citation Number: 189

Abstract

A series of substituted oxindole derivatives was synthesized and evaluated for growth hormone (GH) releasing activity using cultured rat pituitary cells.(+)-6-Carbamoyl-3-(2- chlorophenyl)-(2-diethylaminoethyl)-4-trifluoromethyloxindole (SM-130686, 37S) was found to have potent activity (EC50= 3.0 nM), while the other enantiomer 37R had reduced activity. The absolute configuration of 37S was confirmed by X-ray crystallographic analysis. ...