Naphthalene-1,4-dione compounds possess a wide spectrum of biological activities. In the present study, a series of 1,4-naphthoquinone compounds were synthesized by reacting substituted naphthoquinones with alkyl or aryl amines in presence of a base. The synthesized compounds were screened against Mycobacterium tuberculosis (M. tb) H37Rv, where most of the compounds exhibited significant in vitro antitubercular activities and may serve as a lead for further optimization. Compounds 1, 18, 20 & 25 have IC90 values ranging from 3.14-3.43 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.