Synthesis and structure-activity relationship (SAR) study of 4-azabenzoxazole analogues as H3 antagonists.
The synthesis and SAR of a novel series of 4-azabenzoxazole histamine H(3) antagonists is described. Introduction of substituted phenyl, pyridyl and fused heterocyclic groups to the 6-position of the 4-azabenzoxazole core gave a series of compounds with good H(3) antagonist activity in both ex vivo and in vivo assays.
Chemical Research Department, Department of Chemical Research, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. Ning.shao@merck.com
Ning
N
Shao
Robert
R
Aslanian
Robert E
RE
West
Shirley M
SM
Williams
Ren-Long
RL
Wu
Joyce
J
Hwa
Christopher
C
Sondey
Jean
J
Lachowicz
Anandan
A
Palani
D000818:Animals; D001372:Aza Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D001583:Benzoxazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D054828:Histamine H3 Antagonists / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans; D051379:Mice; D051381:Rats; D018100:Receptors, Histamine H3 / Q000378:metabolism*; D013329:Structure-Activity Relationship
D001372:Aza Compounds; D001583:Benzoxazoles; D054828:Histamine H3 Antagonists; D018100:Receptors, Histamine H3