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Highly active antimycobacterial derivatives of benzoxazine
E. Petrlíková, K. Waisser, H. Divišová, P. Husáková, P. Vrabcová, J. Kuneš, K. Kolář, J. Stolaříková
Bioorganic & medicinal chemistry.
2010 ;
18 (23) :
8178-8187.
[pub] 20101019
Language English Country England, Great Britain
Document type Journal Article, Research Support, Non-U.S. Gov't
Persistent link
https://www.medvik.cz/link/bmc12026684
- 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
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.
References provided by Crossref.org
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- $a Novotná, Eva $7 pna2011673152 $u Department of Inorganic and Organic Chemistry, Charles University in Prague, Hradec Králové, Czech Republic. Eva.Petrlikova@faf.cuni.cz
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