HYPOTENSIVE AND ANTIOXIDANT PROPERTIES OF GAMMA-HYDROXY ACID HYDRAZIDES

Abstract

Abstract A method has been proposed for the preparation of 4-hydroxybutanoic acid hydrazides for the first time. It has been established that the target products are obtained by the interaction of 2-substituted (H, alkyl, aralkyl, allyl, etc.)-4-substituted-4-butanolides with 85% aqueous solution hydrazine hydrate. Testing was carried out on white mongrel mice and reliably shown that the introduction of a hydroxypropyl residue into the composition of the synthesized hydrazides leads to new properties, namely hypotensive activity, not previously observed in compounds class of carboxylic acid hydrazides of various structures. The most active compounds have been selected and tested in rats and cats. It has been established that the lethal dose (lethal doses 50) of the proposed compounds ranges from 550-762 mg/kg and they exhibit superior activity compared to those used in the medical preparation “Dibazol”. In order to find new useful properties in a series of gamma-hydroxy acid hydrazides, their antioxidant features were studied by the method of competitive reactions. As a competitive acceptor, 4-nitroso-N,N-dimethylaniline was used. According to the rate of discoloration of the last the reactivity of H radicals with respect to the studied compounds was determined. H radicals were initiated by photolysis of hydrogen peroxide (conc, 10-3 mol/l), under exposure to ultraviolet radiation, at a wavelength of 313 nm. Initiation rate H radicals were measured by the rate of change in the optical density of para-Nitroso-N,Ndimethyl aniline in distilled water and in the presence of the studied compounds. As a result of the research, it was found that all compounds of this series have antioxidant properties, and some of them are comparable with renowned antioxidant vitamin C.