Back to Search
Start Over
Heteroarylureas with fused bicyclic diamine cores as inhibitors of fatty acid amide hydrolase.
Heteroarylureas with fused bicyclic diamine cores as inhibitors of fatty acid amide hydrolase.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2020 Oct 15; Vol. 30 (20), pp. 127463. Date of Electronic Publication: 2020 Aug 09. - Publication Year :
- 2020
-
Abstract
- A series of mechanism-based heteroaryl urea fatty acid amide hydrolase (FAAH) inhibitors with fused bicyclic diamine cores is described. In contrast to compounds built around a piperazine core, most of the fused bicyclic diamine bearing analogs prepared exhibited greater potency against rFAAH than the human enzyme. Several compounds equipotent against both species were identified and profiled in vivo.<br />Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.<br /> (Copyright © 2020 Elsevier Ltd. All rights reserved.)
- Subjects :
- Amidohydrolases metabolism
Animals
Diamines chemistry
Dose-Response Relationship, Drug
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors chemistry
Humans
Molecular Structure
Rats
Structure-Activity Relationship
Urea analogs & derivatives
Urea chemistry
Amidohydrolases antagonists & inhibitors
Diamines pharmacology
Enzyme Inhibitors pharmacology
Urea pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 30
- Issue :
- 20
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 32784090
- Full Text :
- https://doi.org/10.1016/j.bmcl.2020.127463