Structure-activity relationship studies on tetralin carboxamide growth hormone secretagogue receptor antagonists

Hongyu Zhao; Zhili Xin; Jyoti R Patel; Lissa T J Nelson; Bo Liu; Bruce G Szczepankiewicz; Verlyn G Schaefer; H Douglas Falls; Wiweka Kaszubska; Christine A Collins; Hing L Sham; Gang Liu

doi:10.1016/j.bmcl.2005.02.026

Structure-activity relationship studies on tetralin carboxamide growth hormone secretagogue receptor antagonists

Bioorg Med Chem Lett. 2005 Apr 1;15(7):1825-8. doi: 10.1016/j.bmcl.2005.02.026.

Authors

Hongyu Zhao¹, Zhili Xin, Jyoti R Patel, Lissa T J Nelson, Bo Liu, Bruce G Szczepankiewicz, Verlyn G Schaefer, H Douglas Falls, Wiweka Kaszubska, Christine A Collins, Hing L Sham, Gang Liu

Affiliation

¹ Metabolic Disease Research, Global Pharmaceutical Research and Development, R4MC, AP-10, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA. [email protected]

PMID: 15780615
DOI: 10.1016/j.bmcl.2005.02.026

Abstract

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.

MeSH terms

Administration, Oral
Amides / chemical synthesis*
Amides / pharmacology
Animals
Binding Sites
Biological Availability
Drug Design
Inhibitory Concentration 50
Phenylenediamines / chemistry
Rats
Receptors, G-Protein-Coupled / antagonists & inhibitors*
Receptors, G-Protein-Coupled / metabolism
Receptors, Ghrelin
Structure-Activity Relationship
Tetrahydronaphthalenes / pharmacology*

Substances

Amides
Phenylenediamines
Receptors, G-Protein-Coupled
Receptors, Ghrelin
Tetrahydronaphthalenes
tetralin