Synthesis and biological evaluation of substituted naphthoquinone derivatives as potent antimycobacterial agents

Abstract

In the present study, a series of 1,4-naphthoquinone derivatives were synthesized and screened for antitubercular activity against Mycobacterium tuberculosis H37Rv strain by the broth microdilution assay method. The in vitro antitubercular activity data of the tested compounds against M. tuberculosis strain H37Rv showed moderate to good activity against bacteria compared to reference drugs. The most effective compounds of the series are 26, 28, 29, 34 and 36 with IC50 values ranging from 3.9 - 0.3 μg/mL. The objective of our study is to generate new leads that operate through a different mode of action and to optimize their structure to display potent efficacy. ©ARKAT USA, Inc.