Identification of small molecule agonists of the motilin receptor

被引：14

作者：

Heightman, Tom D. ^{[1
]}

Conway, Elizabeth ^{[2
]}

Corbett, David F. ^{[2
]}

Macdonald, Gregor J. ^{[1
]}

Stemp, Geoffrey

Westaway, Susan M.

Celestini, Paolo ^{[4
]}

Gagliardi, Stefania ^{[4
]}

Riccaboni, Mauro ^{[4
]}

Ronzoni, Silvano ^{[4
]}

Vaidya, Kalindi ^{[2
]}

Butler, Sharon ^{[2
]}

Mckay, Fiona ^{[2
]}

Muir, Alison ^{[2
]}

Powney, Ben ^{[2
]}

Winborn, Kim ^{[2
]}

Wise, Alan ^{[2
]}

Jarvie, Emma M. ^{[1
]}

Sanger, Gareth J. ^{[3
]}

机构：

[1] GlaxoSmithKline, Neurol & GI Ctr Excellence Drug Discovery, Harlow CM19 5AW, Essex, England

[2] GlaxoSmithKline R&D, Mol Discovery Res, Harlow CM19 5AW, Essex, England

[3] GlaxoSmithKline, Med Res Ctr, Immunoinflammat Ctr Excellence Drug Discovery, Stevenage SG1 2NY, Herts, England

[4] NiKem Res Srl, I-20021 Baranzate Di Bollate, MI, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 24期

关键词：

Motilin; Receptor; Agonist; GPCR;

D O I：

10.1016/j.bmcl.2008.10.071

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

High-throughput screening resulted in the identification of a series of novel motilin receptor agonists with relatively low molecular weights. The series originated from an array of biphenyl derivatives designed to target 7-transmembrane (7-TM) receptors. Further investigation of the structure-activity relationship within the series resulted in the identi. cation of compound (22) as a potent and selective agonist at the motilin receptor. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：6423 / 6428

页数：6

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