Benzothiazole derivatives were synthesized and evaluated for their potential as anti-tuberculosis agents. Ten benzothiazole derivatives were docked with isoniazid drug receptors of Mycobacterium tuberculosis and three compounds showed significant inhibitory activity with low binding energies, suggesting drug-likeness. The compounds were characterized using analytical techniques and screened for anti-tubercular activity against the H37Rv strain, with one compound exhibiting significant activity compared to standard drugs.