Identification of small molecule agonists of the motilin receptor

…, S Gagliardi, M Riccaboni, S Ronzoni, K Vaidya…

Index: Heightman, Tom D.; Conway, Elizabeth; Corbett, David F.; Macdonald, Gregor J.; Stemp, Geoffrey; Westaway, Susan M.; Celestini, Paolo; Gagliardi, Stefania; Riccaboni, Mauro; Ronzoni, Silvano; Vaidya, Kalindi; Butler, Sharon; McKay, Fiona; Muir, Alison; Powney, Ben; Winborn, Kim; Wise, Alan; Jarvie, Emma M.; Sanger, Gareth J. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 24 p. 6423 - 6428

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Citation Number: 9

Abstract

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 identification of compound (22) as a potent and selective agonist at the motilin receptor.