Back to Search
Start Over
Fused bicycles as arylketone bioisosteres leading to potent, orally active thiadiazole H3 antagonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 May 01; Vol. 22 (9), pp. 3354-7. Date of Electronic Publication: 2012 Mar 08. - Publication Year :
- 2012
-
Abstract
- A structure-activity relationship study was undertaken to address the lack of oral exposure of the H3 antagonist 1, which incorporated an arylketone. Among a number of sub-series, the 4H-pyrido[1,2-a]pyrimidin-4-one analog 21 showed an improved PK profile in rat and mouse and was active in an obesity model. The pyrimidin-4-one proved to be a novel and useful ketone bioisostere.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 22
- Issue :
- 9
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 22464130
- Full Text :
- https://doi.org/10.1016/j.bmcl.2012.02.076