Highly active antimycobacterial derivatives of benzoxazine
| Autor: | Karel Kolář, Hana Divišová, Jiří Kuneš, Petra Husáková, Karel Waisser, Eva Petrlikova, Petra Vrabcová, Jiřina Stolaříková |
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| Rok vydání: | 2010 |
| Předmět: |
Stereochemistry
medicine.drug_class Clinical Biochemistry Antitubercular Agents Pharmaceutical Science Microbial Sensitivity Tests Antimycobacterial Biochemistry Chemical synthesis Mycobacterium tuberculosis Structure-Activity Relationship Drug Discovery Isoniazid medicine Structure–activity relationship Molecular Biology Antibacterial agent Mycobacterium kansasii biology Chemistry Organic Chemistry biology.organism_classification Benzoxazines Molecular Medicine Mycobacterium avium medicine.drug Mycobacterium |
| Zdroj: | Bioorganic & Medicinal Chemistry. 18:8178-8187 |
| ISSN: | 0968-0896 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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