Phenolic chalcones as agents against Trichomonas vaginalis.
Aldol condensation
Antiprotozoal
Galleria mellonella
Molecular docking
Purine nucleoside phosphorylase
Reactive oxygen species
Trichomoniasis
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
12 2023
12 2023
Historique:
received:
27
12
2022
revised:
12
09
2023
accepted:
25
09
2023
medline:
3
11
2023
pubmed:
16
10
2023
entrez:
15
10
2023
Statut:
ppublish
Résumé
Trichomonas vaginalis, a flagellated and anaerobic protozoan, is a causative agent of trichomoniasis. This disease is among the world's most common non-viral sexually transmitted infection. A single class drug, nitroimidazoles, is currently available for the trichomoniasis treatment. However, resistant isolates have been identified from unsuccessfully treated patients. Thus, there is a great challenge for a discovery of innovative anti-T. vaginalis agents. As part of our ongoing search for antiprotozoal chalcones, we designed and synthesized a series of 21 phenolic chalcones, which were evaluated against T. vaginalis trophozoites. Structure-activity relationship indicated hydroxyl group plays a role key in antiprotozoal activity. 4'-Hydroxychalcone (4HC) was the most active compound (IC
Identifiants
pubmed: 37839143
pii: S0045-2068(23)00549-7
doi: 10.1016/j.bioorg.2023.106888
pii:
doi:
Substances chimiques
4'-hydroxychalcone
2657-25-2
4-hydroxychalcone
20426-12-4
Chalcones
0
Reactive Oxygen Species
0
Antiprotozoal Agents
0
Phenols
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
106888Informations de copyright
Copyright © 2023 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.