Revista medico-chirurgicala a Societatii de Medici si Naturalisti din Iasi · 2008
[Research concerning rutin semisynthetic derivatives. Synthesis, physico-chemical and microbiological characterisation of some new rutin-isoniazid derivatives].
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Lupaşcu D, Tuchiluş Cristina, Profire Lenuţa
Аннотация
UNLABELLED: Isoniazid is one of the most used antituberculosis drugs, but its toxicity is high. In this study, four derivatives of rutin and isoniazid were prepared and their antibacterial and antimycotic activities were investigated.
METHOD: Synthesis of these compounds started through reaction of rutin with fresh prepared sodium methoxide, subsequently treating with 1, 3-dichloro-2-propanol, 1-brom-3-chloropropane, 1, 2-dibrom-ethane or dibrommethane and finally, stirring with isoniazid, to afford crystalline, yellow, water soluble powders.
RESULTS: The four compounds were marginally active against Staphylococcus aureus and Staphylococcus saprophyticus and were inactive against Escherichia coli.
CONCLUSION: We synthesised four new derivatives of rutin and isoniazid; melting points, solubility, yields characterised these compounds, and their structure was confirmed by C, H, N elemental analysis and UV spectra. The compounds showed a modest antibacterial activity. We think that the toxicity of the new derivatives will be lower that of isoniazid toxicity. The next steps in our research will be the toxicological study and antituberculosis assay.
METHOD: Synthesis of these compounds started through reaction of rutin with fresh prepared sodium methoxide, subsequently treating with 1, 3-dichloro-2-propanol, 1-brom-3-chloropropane, 1, 2-dibrom-ethane or dibrommethane and finally, stirring with isoniazid, to afford crystalline, yellow, water soluble powders.
RESULTS: The four compounds were marginally active against Staphylococcus aureus and Staphylococcus saprophyticus and were inactive against Escherichia coli.
CONCLUSION: We synthesised four new derivatives of rutin and isoniazid; melting points, solubility, yields characterised these compounds, and their structure was confirmed by C, H, N elemental analysis and UV spectra. The compounds showed a modest antibacterial activity. We think that the toxicity of the new derivatives will be lower that of isoniazid toxicity. The next steps in our research will be the toxicological study and antituberculosis assay.