A series of 6‐chloro‐3‐(4‐alkylphenyl)‐4‐thioxo‐2H‐1,3‐benzoxazine‐2(3H)‐ones, 7‐chloro‐3‐(4‐alkylphenyl)‐4‐thioxo‐2H‐1,3‐benzoxazine‐2(3H)‐ones, 6‐bromo‐3‐(4‐alkylphenyl)‐4‐thioxo‐2H‐1,3‐benzoxazine‐2(3H)‐ones, 6,8‐dibromo‐3‐(4‐alkylphenyl)‐4‐thioxo‐2H‐1,3‐benzoxazine‐2(3H)‐ones, 6‐chloro‐3‐(4‐alkylphenyl)‐2H‐1,3‐benzoxazine‐2,4(3H)‐dithiones, 7‐chloro‐3‐(4‐alkylphenyl)‐2H‐1,3‐benzoxazine‐2,4(3H)‐dithiones, 6‐bromo‐3‐(4‐alkylphenyl)‐2H‐1,3‐benzoxazine‐2,4(3H)‐dithiones and 6,8‐dibromo‐3‐(4‐alkylphenyl)‐2H‐1,3‐benzoxazine‐2,4(3H)‐dithiones was synthesized. The compounds exhibited in‐vitro activity against Mycobacterium tuberculosis, M. kansasii (two strains), and M. avium. 6‐bromo‐3‐(4‐propylphenyl)‐4‐thioxo‐2H‐1,3‐benzoxazin‐2(3H)‐one and 6‐bromo‐3‐(4‐propylphenyl)‐2H‐1,3‐benzoxazin‐2,4(3H)‐dithione are the most active compounds against M. tuberculosis. The activity is similar to isoniazid (INH). The compounds under study have a broad spectrum of activity against potential pathogenic strains. The replacement of the oxo group by thioxo group of 3‐(4‐alkylphenyl)‐2H‐1,3‐benzoxazine‐2,4(3H)‐diones often led to an improvement in the antimycobacterial activity against M. tuberculosis.

中文翻译：

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高活性潜在抗结核药：3-(4-Alkylphenyl)-4-thioxo-2H-1,3-benzoxazine-2(3H)-ones 和 3-(4-Alkylphenyl)-2H-1,3-benzoxazine-2，环 B 中被卤素取代的 4(3H)-二硫酮

6-氯-3-(4-烷基苯基)-4-硫代-2H-1,3-苯并恶嗪-2(3H)-酮、7-氯-3-(4-烷基苯基)-4-硫代-一系列2H-1,3-苯并恶嗪-2(3H)-ones, 6-bromo-3-(4-烷基苯基)-4-thioxo-2H-1,3-benzoxazine-2(3H)-ones, 6,8-二溴-3-(4-烷基苯基)-4-硫代-2H-1,3-苯并恶嗪-2(3H)-酮、6-氯-3-(4-烷基苯基)-2H-1,3-苯并恶嗪-2 ,4(3H)-dithiones, 7-chloro-3-(4-alkylphenyl)-2H-1,3-benzoxazine-2,4(3H)-dithiones, 6-bromo-3-(4-alkylphenyl)-2H合成了-1,3-苯并恶嗪-2,4(3H)-二硫酮和6,8-二溴-3-(4-烷基苯基)-2H-1,3-苯并恶嗪-2,4(3H)-二硫酮。这些化合物表现出对结核分枝杆菌、堪萨斯分枝杆菌（两种菌株）和鸟分枝杆菌的体外活性。6-溴-3-(4-丙基苯基)-4-硫代-2H-1,3-苯并恶嗪-2(3H)-one和6-溴-3-(4-丙基苯基)-2H-1,3-苯并恶嗪‐2,4(3H)-二硫酮是对抗 M 最活跃的化合物。结核。该活性类似于异烟肼（INH）。所研究的化合物对潜在的致病菌株具有广谱活性。将氧代基团替换为 3-(4-烷基苯基)-2H-1,3-苯并恶嗪-2,4(3H)-二酮的硫代基团通常会提高对结核分枝杆菌的抗分枝杆菌活性。