期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 18, 期 23, 页码 8178-8187出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.10.017
关键词
Benzoxazine; Thioxo group; Antimycobacterial activity; Tuberculosis
资金
- Ministry of Education of the Czech Republic [MSM 0021620822]
- Grant Agency of Charles University [GAUK 11809/2009/B-CH/FAF]
- [SVV-2010-261-001]
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. (C) 2010 Elsevier Ltd. All rights reserved.
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