Discovery and optimization of novel 4-[(aminocarbonyl)amino]-N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists.
This Letter describes optimization of ghrelin receptor antagonists and inverse agonists starting from a screening hit.
Pasternak
Alexander
A
Merck Research Laboratories, Rahway, NJ 07065, USA. alexander_pasternak@merck.com
Goble
Stephen D
SD
deJesus
Reynalda K
RK
Hreniuk
Donna L
DL
Chung
Christine C
CC
Tota
Michael R
MR
Mazur
Paul
P
Feighner
Scott D
SD
Howard
Andrew D
AD
Mills
Sander G
SG
Yang
Lihu
L
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
D019440:Anti-Obesity Agents; D054440:Receptors, Ghrelin; D013449:Sulfonamides; D000096926:Benzenesulfonamides