Novel multitarget 5-arylidenehydantoins with arylpiperazinealkyl fragment: Pharmacological evaluation and investigation of cytotoxicity and metabolic stability.
5-HT(1A)/5-HT(7) modulators
Antidepressant activity
Cytotoxicity
Hydantoin
PDE4 inhibitors
Journal
Bioorganic & medicinal chemistry
ISSN: 1464-3391
Titre abrégé: Bioorg Med Chem
Pays: England
ID NLM: 9413298
Informations de publication
Date de publication:
15 09 2019
15 09 2019
Historique:
received:
16
04
2019
revised:
17
07
2019
accepted:
28
07
2019
pubmed:
7
8
2019
medline:
18
9
2020
entrez:
7
8
2019
Statut:
ppublish
Résumé
On the basis of the structures of serotonin modulators or drugs (NAN-190, buspirone, aripiprazole) and phosphodiesterase 4 (PDE4) inhibitors (rolipram, RO-20-1724), a series of novel multitarget 5-arylidenehydantoin derivatives with arylpiperazine fragment was synthesized. Among these compounds, 5-(3,4-dimethoxybenzylidene-3-(4-(4-(2,3-dichlorophenyl)piperazine-1-yl)butyl)-imidazolidine-2,4-dione (13) and 5-(3-cyclopentyloxy-4-methoxybenzylidene-3-(4-(4-(2-methoxyphenyl)piperazine-1-yl)butyl)-imidazolidine-2,4-dione (18) were found to be the most promising showing very high affinity toward 5-HT
Identifiants
pubmed: 31383628
pii: S0968-0896(19)30639-X
doi: 10.1016/j.bmc.2019.07.046
pii:
doi:
Substances chimiques
Antidepressive Agents
0
Receptors, Serotonin
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
4163-4173Informations de copyright
Copyright © 2019 Elsevier Ltd. All rights reserved.