Department of Inorganic and Organic Chemistry, Charles University in Prague, Hradec Králové, Czech Republic.
Bioorg Med Chem. 2010 Dec 1;18(23):8178-87. doi: 10.1016/j.bmc.2010.10.017. Epub 2010 Oct 19.
New 3-(4-alkylphenyl)-4-thioxo-2H-1,3-benzoxazine-2(3H)-ones and 3-(4-alkylphenyl)-2H-1,3-benzoxazine-2,4(3H)-dithiones were synthesized. The compounds were tested for in vitro antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium avium and two strains of Mycobacterium kansasii. The antimycobacterial activity increased with the replacement of the carbonyl group by the thiocarbonyl group in the starting 3-(4-alkylphenyl)-2H-1,3-benzoxazine-2,4(3H)-diones. The most active derivatives were more active than isonicotinhydrazide (INH). Free-Wilson analysis was also carried out and the activity contribution was examined.
合成了新型 3-(4-烷基苯基)-4-硫代-2H-1,3-苯并恶嗪-2(3H)-酮和 3-(4-烷基苯基)-2H-1,3-苯并恶嗪-2,4(3H)-二硫酮。测试了这些化合物对结核分枝杆菌、鸟分枝杆菌和两种堪萨斯分枝杆菌的体外抗分枝杆菌活性。在起始的 3-(4-烷基苯基)-2H-1,3-苯并恶嗪-2,4(3H)-二酮中，羰基被硫羰基取代后，抗分枝杆菌活性增加。最活跃的衍生物比异烟肼（INH）更有效。还进行了自由-威尔逊分析，并检查了活性贡献。
