Synthesis and structure-activity relationships of isoxazole carboxamides as growth hormone secretagogue receptor antagonists.
A series of isoxazole carboxamide derivatives has been developed as potent ghrelin receptor antagonists. The synthesis and structure-activity relationship (SAR) are described.
Xin
Zhili
Z
Metabolic Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA. zhili.xin@abbott.com
Zhao
Hongyu
H
Serby
Michael D
MD
Liu
Bo
B
Schaefer
Verlyn G
VG
Falls
Douglas H
DH
Kaszubska
Wiweka
W
Colins
Christine A
CA
Sham
Hing L
HL
Liu
Gang
G
D000577:Amides / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D000818:Animals; D001682:Biological Availability; D006801:Humans; D020128:Inhibitory Concentration 50; D007555:Isoxazoles / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology; D008862:Microsomes, Liver / Q000378:metabolism; D051381:Rats; D043562:Receptors, G-Protein-Coupled / Q000037:antagonists & inhibitors*; D054440:Receptors, Ghrelin; D013329:Structure-Activity Relationship
D000577:Amides; D007555:Isoxazoles; D043562:Receptors, G-Protein-Coupled; D054440:Receptors, Ghrelin