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Journal №8 for 2013 г.
Article in number:
Synthesis and study of biological activity of substituted 2-methylenehydrazono-5-aryl-2H-furan-3-ones and their hydrolysis products
Authors:
N.A. Pulina, A.S. Kuznetsov, T.F. Odegova, R.R. Makhmudov
Abstract:
The synthesis of substituted 2-methylenehydrazono-5-aryl-2H-furan-3-ones through reaction of 2-arylfuran-2,3-diones with triphenylphosphoranylidene hydrazones was studied. They are found to hydrolyze to the corresponding hydrazides of 4-aryl-2-hydroxy-4-oxo-2-butenoic acids in the presence of a catalytic amount of hydrochloric acid at 20-25 °C. In heating hydrolysis leads to 5-aryl-2-hydrazono-2H-furan-3-ones and 3-aryl-5-hydroxy-1,6-dihydropyridazine-6-ones. Antimicrobial and anti-inflammatory activity of the synthesized substances was investigated. Active compounds similar to or exceeding the values of the reference drugs were identified. The dependence of the substances - antimicrobial activity on the electron-accepting substituent in aroyl fragment and anti-inflammatory activity on electron-donating group was discovered.
Pages: 3-7
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