Department of Inorganic and Organic Chemistry, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Heyrovský-Str. 1203, 50005 Hradec Králové, Czech Republic.
Eur J Med Chem. 2010 Jul;45(7):2719-25. doi: 10.1016/j.ejmech.2010.02.037. Epub 2010 Feb 20.
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.
合成了新型 3-苄基-4-硫代-2H-1,3-苯并恶嗪-2(3H)-酮和 3-苄基-2H-1,3-苯并恶嗪-2,4(3H)-二硫酮。对这些化合物进行了体外抗结核分枝杆菌活性测试，包括结核分枝杆菌、堪萨斯分枝杆菌和鸟分枝杆菌。将羰基替换为硫代羰基增加了抗分枝杆菌的活性。最具活性的衍生物比异烟肼（INH）更具活性。还研究了细胞毒性和抗增殖活性。
