Discovery of novel pyrrole derivatives as potent agonists for the niacin receptor GPR109A.
GPR109A
Lipolysis
Niacin
Non-esterified fatty acid
Pyrrole
Journal
Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377
Informations de publication
Date de publication:
15 05 2020
15 05 2020
Historique:
received:
29
12
2019
revised:
23
02
2020
accepted:
08
03
2020
pubmed:
23
3
2020
medline:
1
5
2021
entrez:
23
3
2020
Statut:
ppublish
Résumé
Novel pyrrole derivatives were discovered as potent agonists of the niacin receptor, GPR109A. During the derivatization, compound 16 was found to be effective both in vitro and in vivo. The compound 16 exhibited a significant reduction of the non-esterified fatty acid in human GPR109A transgenic rats, and the duration of its in vivo efficacy was much longer than niacin.
Identifiants
pubmed: 32199732
pii: S0960-894X(20)30194-3
doi: 10.1016/j.bmcl.2020.127105
pii:
doi:
Substances chimiques
Fatty Acids, Nonesterified
0
HCAR2 protein, human
0
Nicotinic Agonists
0
Pyrroles
0
Receptors, G-Protein-Coupled
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
127105Informations de copyright
Copyright © 2020 The Authors. Published by Elsevier Ltd.. 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.