Structure-activity relationships of the oxindole growth hormone secretagogues
Structure-activity relationships of the oxindole growth hormone secretagogues
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DOI：
10.1016/j.bmcl.2005.02.042
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发表时间：
2005-04-01
影响因子：
2.7
通讯作者：
Nagata, R
中科院分区：
文献类型：
--
作者：
Tokunaga, T;Hume, WE;Nagata, R
合成了一系列SM-130686的取代氧吲哚衍生物，并对其作为Ghrelin受体激动剂进行了评价。氧化吲哚的C3-芳香族部分的取代基的修饰导致了具有亚纳摩尔结合亲和力的化合物。化合物4I(IC50=0.02 nM)具有低剂量口服活性，口服2 mg/kg，每天2次，连续4天具有体内活性，体重显著增加。(C)2005爱思唯尔有限公司。保留所有权利。
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.