title: Discovery and optimization of novel 4-[(aminocarbonyl)amino]-N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists.
abstract: This Letter describes optimization of ghrelin receptor antagonists and inverse agonists starting from a screening hit.
authors.affiliation: Merck Research Laboratories, Rahway, NJ 07065, USA. alexander_pasternak@merck.com
authors.forename: Alexander
authors.initials: A
authors.lastname: Pasternak
authors.forename: Stephen D
authors.initials: SD
authors.lastname: Goble
authors.forename: Reynalda K
authors.initials: RK
authors.lastname: deJesus
authors.forename: Donna L
authors.initials: DL
authors.lastname: Hreniuk
authors.forename: Christine C
authors.initials: CC
authors.lastname: Chung
authors.forename: Michael R
authors.initials: MR
authors.lastname: Tota
authors.forename: Paul
authors.initials: P
authors.lastname: Mazur
authors.forename: Scott D
authors.initials: SD
authors.lastname: Feighner
authors.forename: Andrew D
authors.initials: AD
authors.lastname: Howard
authors.forename: Sander G
authors.initials: SG
authors.lastname: Mills
authors.forename: Lihu
authors.initials: L
authors.lastname: Yang
mesh_terms: D000818:Animals; D019440:Anti-Obesity Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D015195:Drug Design; D054314:Drug Inverse Agonism; D006801:Humans; D008297:Male; D009765:Obesity / Q000188:drug therapy; D051381:Rats; D017207:Rats, Sprague-Dawley; D054440:Receptors, Ghrelin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000096926:Benzenesulfonamides
chemical_list: D019440:Anti-Obesity Agents; D054440:Receptors, Ghrelin; D013449:Sulfonamides; D000096926:Benzenesulfonamides