Synthesis, in vitro biological evaluation and in silico studies of certain arylnicotinic acids conjugated with aryl (thio)semicarbazides as a novel class of anti-leishmanial agents.
Animals
Antiprotozoal Agents
/ chemical synthesis
Cell Survival
/ drug effects
Chlorocebus aethiops
Dose-Response Relationship, Drug
Leishmania major
/ drug effects
Models, Molecular
Molecular Structure
Nicotinic Acids
/ chemical synthesis
Parasitic Sensitivity Tests
Semicarbazides
/ chemistry
Structure-Activity Relationship
Vero Cells
Anti-amastogite activity
Anti-folate mechanism
Anti-promastigote activity
Arylnicotinic acid - (thio)semicarbazide conjugates
Molecular modeling
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 Oct 2019
01 Oct 2019
Historique:
received:
07
03
2019
revised:
14
06
2019
accepted:
18
06
2019
pubmed:
2
7
2019
medline:
18
10
2019
entrez:
2
7
2019
Statut:
ppublish
Résumé
Herein we introduce new compounds as conjugates of arylnicotinic acids with aryl (thio)semicarbazide derivatives. Based on a structure-guided approach, they were designed to possess anti-leishmanial activity through anti-folate mechanism, via targeting Leishmania major pteridine reductase 1 (Lm-PTR1). The in vitro anti-promastigote and anti-amastigote activity were promising for many thiosemicarbazide derivatives and superior to the reference miltefosine. The most active compounds 8i and 8j exhibited their anti-amastigote activity with IC
Identifiants
pubmed: 31260888
pii: S0223-5234(19)30578-1
doi: 10.1016/j.ejmech.2019.06.051
pii:
doi:
Substances chimiques
Antiprotozoal Agents
0
Nicotinic Acids
0
Semicarbazides
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
335-346Informations de copyright
Copyright © 2019 Elsevier Masson SAS. All rights reserved.