1,4-naphthoquinone structure is common in various natural products and 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, and screened against Mycobacterium tuberculosis (M. tb) H37Rv. Most of the compounds exhibited significant in vitro antitubercular activities and may serve as a lead for further development as a novel class of antituberculosis agents. Compound 9 has IC90 value of 2.40μg/mL. The objective of our study is to generate new leads, as there is an urgent demand for new and more effective anti-TB drugs possessing new modes of action.