Spiro(indoline-3,4′-piperidine) growth hormone secretagogues as ghrelin mimetics

被引：35

作者：

Palucki, BL ^{[1
]}

Feighner, SD

Pong, SS

McKee, KK

Hreniuk, DL

Tan, C

Howard, AD

Van der Ploeg, LHY

Patchett, AA

Nargund, RP

机构：

[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck Res Labs, Dept Obes Res, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(01)00324-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of small molecules derived from MK-0677, a potent synthetic GHS, mimicking the N-terminal Gly-Ser-O-(n-octanoyl)-L-Ser-Phe segment of ghrelin was synthesized and tested in a binding and in a functional assay measuring intracellular calcium elevation in HEK-293 cells expressing hCHSR1a. Replacement of Phe in this tetrapeptide with a spiro(indoline-3,4 '- piperidine) group, Gly-Ser with 2-aminoisobutyric acid, and O-(n-octanoyl)-L-Ser with O-benzyl-D-Ser provided synthetic GHS agonists with similar functional potency as ghrelin. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：1955 / 1957

页数：3

共 5 条

[1] Structure-function studies on the new growth hormone-releasing peptide, ghrelin: Minimal sequence of ghrelin necessary for activation of growth hormone secretagogue receptor 1a [J].