Highly active antimycobacterial derivatives of benzoxazine
Language English Country Great Britain, England Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
21044844
DOI
10.1016/j.bmc.2010.10.017
PII: S0968-0896(10)00939-9
Knihovny.cz E-resources
- MeSH
- Antitubercular Agents chemical synthesis chemistry pharmacology MeSH
- Benzoxazines chemical synthesis chemistry pharmacology MeSH
- Isoniazid pharmacology MeSH
- Microbial Sensitivity Tests MeSH
- Mycobacterium avium drug effects MeSH
- Mycobacterium kansasii drug effects MeSH
- Mycobacterium tuberculosis drug effects MeSH
- Structure-Activity Relationship MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Antitubercular Agents MeSH
- Benzoxazines MeSH
- Isoniazid MeSH
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.
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