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Synthesis and structure-activity relationship (SAR) study of 4-azabenzoxazole analogues as H3 antagonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Mar 01; Vol. 22 (5), pp. 2075-8. Date of Electronic Publication: 2012 Jan 24. - Publication Year :
- 2012
-
Abstract
- 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.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Aza Compounds chemical synthesis
Aza Compounds chemistry
Aza Compounds pharmacokinetics
Aza Compounds pharmacology
Benzoxazoles chemical synthesis
Benzoxazoles pharmacokinetics
Histamine H3 Antagonists chemical synthesis
Histamine H3 Antagonists pharmacokinetics
Humans
Mice
Rats
Structure-Activity Relationship
Benzoxazoles chemistry
Benzoxazoles pharmacology
Histamine H3 Antagonists chemistry
Histamine H3 Antagonists pharmacology
Receptors, Histamine H3 metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 22
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 22326166
- Full Text :
- https://doi.org/10.1016/j.bmcl.2012.01.020