[Research concerning rutin semisynthetic derivatives. Synthesis, physico-chemical and microbiological characterisation of some new rutin-isoniazid derivatives].
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.


METHODS
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.


CONCLUSIONS
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.
Lupaşcu
D
D
Universitatea de Medicină şi Farmacie Gr.T. Popa Iaşi, Facultatea de Farmacie, Disciplina de Chimie Farmaceutică.
Tuchiluş
Cristina
C
Profire
Lenuţa
L
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000494:pharmacology; D003432:Cross-Linking Reagents / Q000138:chemical synthesis; D006801:Humans; D006842:Hydrocarbons, Brominated / Q000138:chemical synthesis; D007538:Isoniazid / Q000138:chemical synthesis* / Q000494:pharmacology*; D000432:Methanol / Q000138:chemical synthesis; D008826:Microbial Sensitivity Tests; D012431:Rutin / Q000138:chemical synthesis* / Q000494:pharmacology*; D013056:Spectrophotometry, Ultraviolet / Q000379:methods; D000517:alpha-Chlorohydrin / Q000031:analogs & derivatives / Q000138:chemical synthesis
D000900:Anti-Bacterial Agents; D000995:Antitubercular Agents; D003432:Cross-Linking Reagents; D006842:Hydrocarbons, Brominated; C033489:1,3-dichloro-2-propanol; D012431:Rutin; D000517:alpha-Chlorohydrin; C050753:1,2-dibromopropane; C027947:methylene bromide; D007538:Isoniazid; D000432:Methanol