Evaluation of New Benzimidazole Derivatives as Cysticidal Agents: In Vitro, in Vivo and Docking Studies.
benzimidazole derivative
in vitro cysticidal activity
in vivo cysticidal activity
molecular modeling
pharmacokinetics
Journal
Chemical & pharmaceutical bulletin
ISSN: 1347-5223
Titre abrégé: Chem Pharm Bull (Tokyo)
Pays: Japan
ID NLM: 0377775
Informations de publication
Date de publication:
2019
2019
Historique:
entrez:
3
12
2019
pubmed:
4
12
2019
medline:
16
1
2020
Statut:
ppublish
Résumé
Based on our previous research on cysticidal drugs, we report the synthesis and evaluation of three new benzimidazole derivatives. In these compounds, the amido group was used as a bioisosteric replacement of the ester group. The molecular docking on β-tubulin revealed that the derivatives interacted through hydrogen bonding with N165, E198 and V236. All compounds showed in vitro activity against Taenia crassiceps cysts. Among them, benzimidazole 3 was found to be the most potent of the series (EC
Identifiants
pubmed: 31787656
doi: 10.1248/cpb.c19-00574
doi:
Substances chimiques
Amebicides
0
Benzimidazoles
0
benzimidazole
E24GX49LD8
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM