Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 1.
SAR studies for novel non-imidazole containing H(3) receptor antagonists with high potency and selectivity for rat H(3) receptors are described. A high throughput screening lead, A-923, was further elaborated in a systematic manner to clarify a pharmacophore for this class of aryloxyalkyl piperazine based compounds.
Faghih
Ramin
R
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064-6123, USA. ramin.faghih@abbott.com
Dwight
Wesley
W
Gentles
Robert
R
Phelan
Kathleen
K
Esbenshade
Timothy A
TA
Ireland
Lynne
L
Miller
Thomas R
TR
Kang
Chae-Hee
CH
Fox
Gerard B
GB
Gopalakrishnan
Sujatha M
SM
Hancock
Arthur A
AA
Bennani
Youssef L
YL
D000588:Amines / Q000737:chemistry; D000818:Animals; D001667:Binding, Competitive; D002219:Carbamates / Q000737:chemistry; D002540:Cerebral Cortex / Q000378:metabolism; D006633:Histamine Antagonists / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D006801:Humans; D007659:Ketones / Q000737:chemistry*; D007700:Kinetics; D008024:Ligands; D010879:Piperazines / Q000737:chemistry*; D051381:Rats; D011969:Receptors, Histamine H1 / Q000378:metabolism; D011970:Receptors, Histamine H2 / Q000378:metabolism; D018100:Receptors, Histamine H3 / Q000187:drug effects* / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
C470892:A-923 compound; D000588:Amines; D002219:Carbamates; D006633:Histamine Antagonists; D007659:Ketones; D008024:Ligands; D010879:Piperazines; D011969:Receptors, Histamine H1; D011970:Receptors, Histamine H2; D018100:Receptors, Histamine H3