A note to the biological activity of benzoxazine derivatives containing the thioxo group

New 3-benzyl-4-thioxo-2H-1,3-benzoxazine-2(3H)-ones and 3-benzyl-2H-1,3-benzoxazine-2,4(3H)-dithiones were synthesized. The compounds were tested for in vitro antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium kansasii and Mycobacterium avium. The replacement of the carbonyl group by the thiocarbonyl group increased the antimycobacterial activity. The most active derivatives were more active than isonicotinhydrazide (INH). The cytotoxicity and the antiproliferative activity were studied as well.

Graphical abstractThe replacement of the oxo group by the thioxo group in 3-benzyl-2H-1,3-benzoxazine-2,4(3H)-diones [1] increases antimycobacterial activity. The most active derivatives are more active than isonicotinhydrazide (INH).Figure optionsDownload full-size imageDownload as PowerPoint slide