Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists

Gregory A Gfesser; Henry Zhang; Jurgen Dinges; Gerard B Fox; Jia Bao Pan; Timothy A Esbenshade; Betty B Yao; David Witte; Thomas R Miller; Chae-Hee Kang; Kathy M Krueger; Youssef L Bennani; Arthur A Hancock; Ramin Faghih

doi:10.1016/j.bmcl.2003.11.038

Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists

Bioorg Med Chem Lett. 2004 Feb 9;14(3):673-6. doi: 10.1016/j.bmcl.2003.11.038.

Authors

Gregory A Gfesser¹, Henry Zhang, Jurgen Dinges, Gerard B Fox, Jia Bao Pan, Timothy A Esbenshade, Betty B Yao, David Witte, Thomas R Miller, Chae-Hee Kang, Kathy M Krueger, Youssef L Bennani, Arthur A Hancock, Ramin Faghih

Affiliation

¹ Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA. greg.gfesser@abbott.com

PMID: 14741266
DOI: 10.1016/j.bmcl.2003.11.038

Abstract

Further SAR studies on novel histamine H(3) receptor antagonists are presented. Compound 14bb is a potent antagonist of both the rat cortical and human clone receptors, and is demonstrated to act functionally as an antagonist in an in vivo mouse dipsogenia model.

MeSH terms

Animals
Histamine Antagonists / chemistry*
Histamine Antagonists / pharmacology*
Humans
Ligands
Mice
Models, Animal
Molecular Structure
Oxadiazoles / chemistry*
Oxadiazoles / pharmacology*
Rats
Receptors, Histamine H3 / chemistry*
Receptors, Histamine H3 / drug effects*
Receptors, Histamine H3 / metabolism
Structure-Activity Relationship

Substances

Histamine Antagonists
Ligands
Oxadiazoles
Receptors, Histamine H3