Mycobactin Analogues with Excellent Pharmacokinetic Profile Demonstrate Potent Antitubercular Specific Activity and Exceptional Efflux Pump Inhibition.
Animals
Antitubercular Agents
/ chemistry
Bacterial Proteins
/ antagonists & inhibitors
Calcium Channel Blockers
/ pharmacology
Ion Transport
Iron Chelating Agents
/ pharmacology
Male
Membrane Transport Proteins
/ chemistry
Mycobacterium tuberculosis
/ drug effects
Oxazoles
/ chemistry
Rats
Rats, Sprague-Dawley
Tissue Distribution
Tuberculosis
/ drug therapy
Verapamil
/ pharmacology
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
13 01 2022
13 01 2022
Historique:
pubmed:
5
1
2022
medline:
8
2
2022
entrez:
4
1
2022
Statut:
ppublish
Résumé
In this study, we have designed and synthesized pyrazoline analogues that partially mimic the structure of mycobactin, to address the requirement of novel therapeutics to tackle the emerging global challenge of antimicrobial resistance (AMR). Our investigation resulted in the identification of novel lead compounds
Identifiants
pubmed: 34981940
doi: 10.1021/acs.jmedchem.1c01349
doi:
Substances chimiques
Antitubercular Agents
0
Bacterial Proteins
0
Calcium Channel Blockers
0
Iron Chelating Agents
0
Membrane Transport Proteins
0
Oxazoles
0
mycobactins
0
Verapamil
CJ0O37KU29
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
234-256Subventions
Organisme : Medical Research Council
ID : G0802079
Pays : United Kingdom