Structure-activity relationship studies on tetralin carboxamide growth hormone secretagogue receptor antagonists.
The structure-activity relationship studies on a series of tetralin carboxamide growth hormone secretagogue receptor (GHS-R) antagonists are discussed. It was found that certain 2-alkoxycarbonylamino substituted tetralin carboxamides are potent, selective, and orally bioavailable GHS-R antagonists.
Zhao
Hongyu
H
Metabolic Disease Research, Global Pharmaceutical Research and Development, R4MC, AP-10, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA. hongyu.zhao@abbott.com
Xin
Zhili
Z
Patel
Jyoti R
JR
Nelson
Lissa T J
LT
Liu
Bo
B
Szczepankiewicz
Bruce G
BG
Schaefer
Verlyn G
VG
Falls
H Douglas
HD
Kaszubska
Wiweka
W
Collins
Christine A
CA
Sham
Hing L
HL
Liu
Gang
G
D000284:Administration, Oral; D000577:Amides / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D001665:Binding Sites; D001682:Biological Availability; D015195:Drug Design; D020128:Inhibitory Concentration 50; D010655:Phenylenediamines / Q000737:chemistry; D051381:Rats; D043562:Receptors, G-Protein-Coupled / Q000037:antagonists & inhibitors* / Q000378:metabolism; D054440:Receptors, Ghrelin; D013329:Structure-Activity Relationship; D013764:Tetrahydronaphthalenes / Q000494:pharmacology*
D000577:Amides; D010655:Phenylenediamines; D043562:Receptors, G-Protein-Coupled; D054440:Receptors, Ghrelin; D013764:Tetrahydronaphthalenes; C095210:tetralin