Synthesis and antimycobacterial activity of 1,2,4-triazole 3-benzylsulfanyl derivatives
Autor: | Jarmila Kaustová, Ute Möllmann, Lenka Zahajska, Věra Klimešová, Karel Waisser |
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Rok vydání: | 2003 |
Předmět: |
chemistry.chemical_classification
Mesylates Chemistry medicine.drug_class Stereochemistry Pharmaceutical Science 1 2 4-Triazole Microbial Sensitivity Tests Mycobacterium tuberculosis Alkylation Triazoles Antimycobacterial Anti-Bacterial Agents Minimum inhibitory concentration chemistry.chemical_compound Drug Discovery Mycobacterium kansasii Nitro medicine Moiety Humans Cytotoxicity Thioamide Mycobacterium avium |
Zdroj: | Farmaco (Societa chimica italiana : 1989). 59(4) |
ISSN: | 0014-827X |
Popis: | Series of 3-benzylsulfanyl derivatives of 1,2,4-triazole and 4-methyl-1,2,4-triazole were synthesized by alkylation of starting triazole-3-thiol with appropriately substituted benzyl halide. All members of the set were evaluated for in vitro antimycobacterial activity against Mycobacterium tuberculosis, M. avium, and two strains of M. kansasii. The activities were expressed as the minimum inhibitory concentration. The compounds exhibited only a moderate or slight antimycobacterial activity. Minimum inhibitory concentrations fall into a range of 32-1000 micromol/l. The most active substances bear two nitro groups or a thioamide group on the benzyl moiety. As regards the cytotoxicity effect, the evaluated compounds can be considered as moderately toxic. |
Databáze: | OpenAIRE |
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