Synthesis and biological evaluation of naphthalene-1,4-dione derivatives as potent antimycobacterial agents.
The recent increase in the incidence of tuberculosis with the emergence of multi-drug resistant (MDR) cases has lead to the search for new drugs that are effective against MDR strains of Mycobacterium tuberculosis (M. tb) and can augment the potential of existing drugs against tuberculosis. In the present study a series of naphthalene-1,4-dione derivatives were synthesized and evaluated for their in vitro antimycobacterial activity against M. tb H37Rv strain. Preliminary results indicated that most of the compounds demonstrated significant antimycobacterial activities. The most effective compounds of the series 7, 8 and 10 have MIC values of 3.13 microg/mL and growth inhibition of 99%. Compound 7 has an IC50 value of 0.49 microg/mL. Compounds 1, 3 and 18 with MIC values of 3.13 microg/mL also showed 96-98% growth inhibition. The objective of our study is to generate new leads through different mode of action and to optimize their structure to display the potent efficacy.
Mital
A
A
Department of Pharmaceutical Technology, National Institute of Pharmaceutical Education and Research, Sector 67, S. A. S. Nagar-160062, Punjab, India. alkamital@gmail.com
Negi
V S
VS
Ramachandran
U
U
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects* / Q000254:growth & development; D009285:Naphthoquinones / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D018088:Tuberculosis, Multidrug-Resistant
D000900:Anti-Bacterial Agents; D009285:Naphthoquinones