Synthesis and antituberculosis activity of 5-methyl/trifluoromethoxy-1H-indole-2,3-dione 3-thiosemicarbazone derivatives
| Autor: | Aydın Salman, Özlen Güzel, Nilgün Karalı |
|---|---|
| Rok vydání: | 2008 |
| Předmět: |
Thiosemicarbazones
Indoles Stereochemistry Clinical Biochemistry Antitubercular Agents Pharmaceutical Science Microbial Sensitivity Tests Biochemistry Chemical synthesis Mycobacterium tuberculosis Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Structure–activity relationship Molecular Biology Semicarbazone Antibacterial agent Indole test biology Bicyclic molecule Organic Chemistry biology.organism_classification chemistry Lactam Molecular Medicine |
| Zdroj: | Bioorganic & Medicinal Chemistry. 16:8976-8987 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2008.08.050 |
| Popis: | New series of 5-methyl/trifluoromethoxy-1H-indole-2,3-dione 3-thiosemicarbazones 3a-t, 1-methyl-5-methyl/trifluoromethoxy-1H-indole-2,3-dione 3-thiosemicarbazones 4a-y and 5-trifluoromethoxy-1-morpholinomethyl-1H-indole-2,3-dione 3-thiosemicarbazones 5a-m were synthesized. The structures of the synthesized compounds were confirmed by spectral data and elemental analysis. The new 5-methyl/trifluoromethoxy-1H-indole-2,3-dione derivatives, along with previously synthesized 5-methyl-1H-indole-2,3-dione 3-thiosemicarbazones 6a-l, were evaluated for in vitro antituberculosis activity against Mycobacterium tuberculosis H37Rv. 5-Methyl-1H-indole-2,3-dione 3-thiosemicarbazones (3b, 3d, 3f, 6c, 6d, and 6f), 5-trifluoromethoxy-1H-indole-2,3-dione 3-thiosemicarbazones (3q-s) and 5-trifluoromethoxy-1-morpholinomethyl-1H-indole-2,3-dione 3-thiosemicarbazones (5e and 5j-l) were found to be the most potent inhibitors of M. tuberculosis growth described in this study. |
| Databáze: | OpenAIRE |
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