title: Potent achiral agonists of the growth hormone secretagogue (ghrelin) receptor. Part 2: Lead optimisation.
abstract: A series of small molecule orally bioavailable ghrelin receptor agonists have been identified through systematic optimisation of a high throughput screening hit.
authors.affiliation: Department of Medicinal Chemistry & DMPK, Neurology & GI Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. Jason_Witherington@GSK.com
authors.forename: Jason
authors.initials: J
authors.lastname: Witherington
authors.forename: Lee
authors.initials: L
authors.lastname: Abberley
authors.forename: Michael A
authors.initials: MA
authors.lastname: Briggs
authors.forename: Katharine
authors.initials: K
authors.lastname: Collis
authors.forename: David K
authors.initials: DK
authors.lastname: Dean
authors.forename: Alessandra
authors.initials: A
authors.lastname: Gaiba
authors.forename: N Paul
authors.initials: NP
authors.lastname: King
authors.forename: Helmut
authors.initials: H
authors.lastname: Kraus
authors.forename: Nicola
authors.initials: N
authors.lastname: Shuker
authors.forename: Jon G A
authors.initials: JG
authors.lastname: Steadman
authors.forename: Andrew K
authors.initials: AK
authors.lastname: Takle
authors.forename: Gareth
authors.initials: G
authors.lastname: Sanger
authors.forename: Graham
authors.initials: G
authors.lastname: Wadsworth
authors.forename: Sharon
authors.initials: S
authors.lastname: Butler
authors.forename: Fiona
authors.initials: F
authors.lastname: McKay
authors.forename: Alison
authors.initials: A
authors.lastname: Muir
authors.forename: Kim
authors.initials: K
authors.lastname: Winborn
authors.forename: Tom D
authors.initials: TD
authors.lastname: Heightman
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D005453:Fluorescence; D007211:Indoles / Q000138:chemical synthesis / Q000494:pharmacology*; D008297:Male; D015394:Molecular Structure; D051381:Rats; D017207:Rats, Sprague-Dawley; D044302:Receptor, Serotonin, 5-HT1B / Q000378:metabolism; D054440:Receptors, Ghrelin / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D007211:Indoles; D044302:Receptor, Serotonin, 5-HT1B; D054440:Receptors, Ghrelin; C529346:SB-791016; D013449:Sulfonamides