SYNTHESIS AND BIOLOGICAL EVALUATION
OF SOME NEW RUTIN SEMISYNTHETIC
DERIVATIVES AS ANTIBACTERIAL AGENTS
DAN LUPAŞCU1*, CRISTINA TUCHILUŞ2, CĂTĂLINA ELENA
LUPUŞORU3, CRISTINA GHICIUC3, MARIA ŞUTU1, ALEXANDRA
NEAGU1, LENUŢA PROFIRE1
1Pharmaceutical Chemistry Department, 2Microbiology Department,
Faculty of Pharmacy; 3Pharmacology and Toxicology Department,
Faculty of Medicine, „Gr. T. Popa” University of Medicine and
Pharmacy, Universităţii Street, 16, 700115, Iaşi, Romania
*corresponding author: danlup69@yahoo.com
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Abstract:

Many studies show that flavonoids have a lot of biological properties, including the antimicrobial effect. It is also known that rutin is able to increase the antibacterial activity of other compounds. On the other hand, the antibacterial sulphonamides have weak water solubility, which is responsible for the renal serious secondary effects. Starting from
these facts, we synthesised some water soluble rutin derivatives with antibacterial sulphonamides, treating rutin with 1,3-dichloro-2-propanol, 1-bromo-3-chloro-propane, 2- dibromethane and dibrommethane, and then with sulfadimethoxyne, sulfamethoxazole, sulfachloropyridazine, sulfapyridine, sulfisoxazole, sulfacetamide, sulfadiazine, sulfamerazine, sulfathiazole. Molecular formula, weight, yield, melting points and
solubility have characterized the new derivatives. Elemental analysis and spectral analysis (UV and IR) have confirmed the structure of the new compounds. In vitro and in vivo microbiological assays were performed. Some of them showed marked antibacterial properties. The most active compounds are the sulfapyridine and sulfachloropyridazine derivatives, that have an equal activity or are even more active than cotrimoxazole

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