Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists.
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.
Gfesser
Gregory A
GA
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA. greg.gfesser@abbott.com
Zhang
Henry
H
Dinges
Jurgen
J
Fox
Gerard B
GB
Pan
Jia Bao
JB
Esbenshade
Timothy A
TA
Yao
Betty B
BB
Witte
David
D
Miller
Thomas R
TR
Kang
Chae-Hee
CH
Krueger
Kathy M
KM
Bennani
Youssef L
YL
Hancock
Arthur A
AA
Faghih
Ramin
R
D000818:Animals; D006633:Histamine Antagonists / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D008024:Ligands; D051379:Mice; D023421:Models, Animal; D015394:Molecular Structure; D010069:Oxadiazoles / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D018100:Receptors, Histamine H3 / Q000737:chemistry* / Q000187:drug effects* / Q000378:metabolism; D013329:Structure-Activity Relationship
D006633:Histamine Antagonists; D008024:Ligands; D010069:Oxadiazoles; D018100:Receptors, Histamine H3