The fatty acid amide hydrolase and cyclooxygenase-inhibitory properties of novel amide derivatives of carprofen.
Carprofen
Carprofen amides
Cyclooxygenase
Endocannabinoid
FAAH inhibition
Fatty acid amide hydrolase
Non-steroidal anti-inflammatory drugs
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
08 2020
08 2020
Historique:
received:
05
04
2020
revised:
05
06
2020
accepted:
15
06
2020
pubmed:
1
7
2020
medline:
19
3
2021
entrez:
30
6
2020
Statut:
ppublish
Résumé
In experimental animals, inhibition of fatty acid amide hydrolase (FAAH) reduces the gastrointestinal damage produced by non-steroidal anti-inflammatory agents that act by inhibition of cyclooxygenase (COX). This suggests that compounds able to inhibit both enzymes may be potentially useful therapeutic agents. In the present study, we have investigated eight novel amide analogues of carprofen, ketoprofen and fenoprofen as potential FAAH/COX dual action inhibitors. Carpro-AM1 (2-(6-Chloro-9H-carbazol-2-yl)-N-(3-methylpyridin-2-yl)propenamide) and Carpro-AM6 (2-(6-Chloro-9H-carbazol-2-yl)-N-(3-chloropyridin-2-yl)propenamide) were found to be fully reversible inhibitors of the hydrolysis of 0.5 µM [
Identifiants
pubmed: 32599361
pii: S0045-2068(20)31331-6
doi: 10.1016/j.bioorg.2020.104034
pii:
doi:
Substances chimiques
Anti-Inflammatory Agents, Non-Steroidal
0
Carbazoles
0
Cyclooxygenase Inhibitors
0
Amidohydrolases
EC 3.5.-
fatty-acid amide hydrolase
EC 3.5.1.-
carprofen
FFL0D546HO
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
104034Commentaires et corrections
Type : ErratumIn
Informations de copyright
Copyright © 2020 Elsevier Inc. All rights reserved.
Déclaration de conflit d'intérêts
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.