Benzimidazoquinazolines as new potent anti-TB chemotypes: Design, synthesis, and biological evaluation.
Animals
Antitubercular Agents
/ chemical synthesis
Benzimidazoles
/ chemical synthesis
Cell Survival
/ drug effects
Dose-Response Relationship, Drug
Drug Design
Mice
Microbial Sensitivity Tests
Molecular Structure
Mycobacterium tuberculosis
/ drug effects
Quinazolines
/ chemical synthesis
RAW 264.7 Cells
Structure-Activity Relationship
Tuberculosis
/ drug therapy
Anti-TB (H37Rv) activity
Benzimidazoquinolines
INH resistant-Mtb
New anti-TB chemotypes
Polyheterocycle
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
06 2020
06 2020
Historique:
received:
11
02
2020
accepted:
16
03
2020
pubmed:
1
4
2020
medline:
24
2
2021
entrez:
1
4
2020
Statut:
ppublish
Résumé
In search for new molecular entities as anti-TB agents, the benzimidazoquinazoline polyheterocyclic scaffold has been designed adopting the scaffold hopping strategy. Thirty-two compounds have been synthesized through an improved tandem decarboxylative nucleophilic addition cyclocondensation reaction of o-phenylenediamine with isatoic anhydride followed by further cyclocondensation of the intermediately formed 2-(o-aminoaryl)benzimidazole with trialkyl orthoformate/acetate. The resultant benzimidazoquinazolines were evaluated in vitro for anti-TB activity against M. tuberculosis H
Identifiants
pubmed: 32224336
pii: S0045-2068(20)30342-4
doi: 10.1016/j.bioorg.2020.103774
pii:
doi:
Substances chimiques
Antitubercular Agents
0
Benzimidazoles
0
Quinazolines
0
benzimidazole
E24GX49LD8
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
103774Informations de copyright
Copyright © 2020 Elsevier Inc. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of Competing Interest The authors declare no competing financial interest.