Design, synthesis and biological evaluation of substituted 2-amino-1,3-thiazine derivatives as antituberculosis and anti-cancer agents

<p>A series of substituted 2-amino-1,3-thiazines were synthesized as amides (<b>9a–9i</b>), carbamates (<b>9j–9m</b>), sulfonamides (<b>9n–9o</b>) and urea derivatives (<b>9p–9q</b>) by treating the compound <b>7</b> with acid chlorides (<b>8a–8i</b>), chloroformates (<b>8j–8m</b>), sulfonyl chlorides (<b>8n–8o</b>) and isocyanates (<b>8p–8q</b>) respectively. The synthesized compounds (<b>9a–9q</b>) were screened for <i>antituberculosis</i> activity against <i>Mycobacterium tuberculosis</i> H<sub>37</sub>Rv ATCC 27294 and the results show that some of these derivatives possess good activity against <i>Mycobacterium tuberculosis</i> H<sub>37</sub>Rv ATCC 27294. A few also display promising cytotoxic activity against human breast cancer MCF-7 and human esophageal cancer EC-9706 cell lines. Regarding both biological profiles <b>9b, 9m</b> and <b>9h</b> are the most active for anti-cancer, anti-TB activity.</p>