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

作者:Waisser Karel*; Petrlikova Eva; Perina Milan; Klimesova Vera; Kunes Jiri; Palat Karel Jr; Kaustova Jarmila; Dahse Hans Martin; Moellmann Ute
来源:European Journal of Medicinal Chemistry, 2010, 45(7): 2719-2725.
DOI:10.1016/j.ejmech.2010.02.037

摘要

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.

  • 出版日期2010-7