Biological evaluation of novel curcumin-pyrazole-mannich derivative active against drug-resistant Mycobacterium tuberculosis.
Future Microbiol
; 12: 1349-1362, 2017 11.
Article
in En
| MEDLINE
| ID: mdl-29035081
ABSTRACT
AIM:
Our objective was to identify a more potent curcumin derivative with specific activity against Mycobacterium tuberculosis. MATERIALS &METHODS:
A total of 21 curcumin derivatives were synthesized and detailed bio-evaluation was carried out including determination of static/cidality, synergy with front-line antituberculosis drugs and determination of efficacy in the murine model of M. tuberculosis infection.RESULTS:
We identified CPMD-6d dihydrochloride exhibiting concentration-dependent bactericidal activity against M. tuberculosis (MIC 2 µg/ml), even against drug-resistant strains. In addition, it synergizes with front-line antituberculosis drugs as well as significantly reduces bacterial load in mice lungs and spleen at 25 mg/kg as compared with ethambutol at 100 mg/kg.CONCLUSION:
Taken together, CPMD-6d dihydrochloride exhibits all properties to be positioned as a novel molecule of interest for treatment of tuberculosis. Graphical abstract [Formula see text].Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Pyrazoles
/
Tuberculosis, Multidrug-Resistant
/
Curcumin
/
Mannich Bases
/
Mycobacterium tuberculosis
/
Antitubercular Agents
Type of study:
Prognostic_studies
Limits:
Animals
/
Female
/
Humans
Language:
En
Journal:
Future Microbiol
Journal subject:
MICROBIOLOGIA
Year:
2017
Document type:
Article
Affiliation country:
India