Quinazoline and phthalazine derivatives as novel melatonin receptor ligands analogues of agomelatine.
Agomelatine
Agonist
MT(1)
MT(2)
Melatonin receptor
Phthalazine
Quinazoline
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
01 Mar 2020
01 Mar 2020
Historique:
received:
01
09
2019
revised:
12
11
2019
accepted:
16
01
2020
pubmed:
1
2
2020
medline:
31
10
2020
entrez:
1
2
2020
Statut:
ppublish
Résumé
For further development of successors of Agomelatine through modulation of its pharmacokinetic properties, we report herein the design, synthesis and pharmacological results of a new family of melatonin receptor ligands. Issued from the introduction of quinazoline and phthalazine scaffolds carrying an ethyl amide lateral chain and a methoxy group as bioisosteric ligands analogues of previously developed Agomelatine. The biological activity of the prepared analogues was compared with that of Agomelatine. Quinazoline and phthalazine rings proved to be a versatile scaffold for easy feasible MT
Identifiants
pubmed: 32004937
pii: S0223-5234(20)30045-3
doi: 10.1016/j.ejmech.2020.112078
pii:
doi:
Substances chimiques
Acetamides
0
Ligands
0
Phthalazines
0
Quinazolines
0
Receptor, Melatonin, MT1
0
Receptor, Melatonin, MT2
0
agomelatine
137R1N49AD
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
112078Informations de copyright
Copyright © 2020 Elsevier Masson SAS. 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.