Synthesis and structure-activity relationships of isoxazole carboxamides as growth hormone secretagogue receptor antagonists

Zhili Xin; Hongyu Zhao; Michael D Serby; Bo Liu; Verlyn G Schaefer; Douglas H Falls; Wiweka Kaszubska; Christine A Colins; Hing L Sham; Gang Liu

doi:10.1016/j.bmcl.2004.11.075

Synthesis and structure-activity relationships of isoxazole carboxamides as growth hormone secretagogue receptor antagonists

Bioorg Med Chem Lett. 2005 Feb 15;15(4):1201-4. doi: 10.1016/j.bmcl.2004.11.075.

Authors

Zhili Xin¹, Hongyu Zhao, Michael D Serby, Bo Liu, Verlyn G Schaefer, Douglas H Falls, Wiweka Kaszubska, Christine A Colins, Hing L Sham, Gang Liu

Affiliation

¹ Metabolic Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA. zhili.xin@abbott.com

PMID: 15686942
DOI: 10.1016/j.bmcl.2004.11.075

Abstract

A series of isoxazole carboxamide derivatives has been developed as potent ghrelin receptor antagonists. The synthesis and structure-activity relationship (SAR) are described.

MeSH terms

Amides / chemical synthesis*
Amides / metabolism
Amides / pharmacology
Animals
Biological Availability
Humans
Inhibitory Concentration 50
Isoxazoles / chemical synthesis
Isoxazoles / metabolism
Isoxazoles / pharmacology
Microsomes, Liver / metabolism
Rats
Receptors, G-Protein-Coupled / antagonists & inhibitors*
Receptors, Ghrelin
Structure-Activity Relationship

Substances

Amides
Isoxazoles
Receptors, G-Protein-Coupled
Receptors, Ghrelin