Design, synthesis and biological activity of N-(2-phenoxy)ethyl imidazo[1,2-a]pyridine-3-carboxamides as new antitubercular agents.
Animals
Antitubercular Agents
/ administration & dosage
Dose-Response Relationship, Drug
Drug Design
Female
Imidazoles
/ administration & dosage
Mice
Mice, Inbred ICR
Microbial Sensitivity Tests
Molecular Structure
Mycobacterium tuberculosis
/ drug effects
Pyridines
/ administration & dosage
Structure-Activity Relationship
Antimycobacterial activity
Design
Synthesis
imidazo[1,2-a]pyridine
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:
15 Sep 2019
15 Sep 2019
Historique:
received:
29
03
2019
revised:
13
06
2019
accepted:
13
06
2019
pubmed:
24
6
2019
medline:
8
10
2019
entrez:
24
6
2019
Statut:
ppublish
Résumé
A series of N-(2-phenoxy)ethyl imidazo[1,2-a]pyridine-3-carboxamides (IPAs), based on the structure of WZY02 discovered in our lab, were designed and synthesized as new anti-TB agents. Results reveal that many of them exhibit excellent in vitro inhibitory activity with low nanomolar MIC values against both drug-sensitive MTB strain H37Rv and drug-resistant clinical isolates. Compounds 15b and 15d display good safety and pharmacokinetic profiles, suggesting their promising potential to be lead compounds for future antitubercular drug discovery.
Identifiants
pubmed: 31229874
pii: S0223-5234(19)30565-3
doi: 10.1016/j.ejmech.2019.06.038
pii:
doi:
Substances chimiques
Antitubercular Agents
0
Imidazoles
0
Pyridines
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
715-725Informations de copyright
Copyright © 2019 Elsevier Masson SAS. All rights reserved.