Back to Search
Start Over
Design, synthesis and SAR of a novel series of benzimidazoles as potent NPY Y5 antagonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Dec 01; Vol. 20 (23), pp. 7120-3. Date of Electronic Publication: 2010 Sep 17. - Publication Year :
- 2010
-
Abstract
- A novel class of benzimidazole NPY Y5 receptor antagonists was prepared exploiting a privileged spirocarbamate moiety. The structure-activity relationship of this series and efforts to achieve a profile suitable for further development and an appropriate pharmacokinetic profile in rat are described. Optimisation led to the identification of the brain penetrant, orally bioavailable Y5 antagonist 9b which significantly inhibited the food intake induced by a Y5 selective agonist with a minimal effective dose of 30mg/kg po.<br /> (Copyright © 2010 Elsevier Ltd. All rights reserved.)
- Subjects :
- Administration, Oral
Animals
Benzimidazoles chemical synthesis
Benzimidazoles pharmacokinetics
Brain metabolism
Dose-Response Relationship, Drug
Rats
Structure-Activity Relationship
Benzimidazoles chemistry
Benzimidazoles pharmacology
Drug Design
Eating drug effects
Receptors, Neuropeptide Y antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 20
- Issue :
- 23
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 20951033
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.09.064