SYNTHESIS, ANALGESIC AND ANTIMICROBIAL ACTIVITY OF N-HETARYLAMIDESOF 2-(2-(DIARYLMETHYLENE)HYDRAZONO)-5,5-DIMETHYL-4-OXOHEXANOIC ACID

New N-hetaryl substituted 2-((diarylmethylene)hydrazono)-5,5-dimethyl-4-oxohexana-mides were obtained in 4 steps: a) Claisen condensation between pinacolone and diethyl oxalate in the presence of sodium methylate; b) the condensation of pivaloyl pyruvic acid with diarylmethylene hydrazones to form 2-diarylmethylenehydrazono-4-oxo-5,5-dimethylhexanoic acid; c) intramolecular cyclization of hydrazonoacids in hydrazonofuranones; d) decyclization of the latter under the action of heterocyclic amines. Isolation of N-hetaryl-2-((diarylmethylene)hydrazono)-5,5-dimethyl-4-oxohexanamides was carried out by filtration of the resulting precipitate with subsequent recrystallization from ethanol or propane-2-ol. The structure of the obtained compounds was con-firmed by the methods of H-1 and C-13 NMR spectroscopy and elemental analysis. It is established that the obtained substituted hetarylamides exist in solutions of deuterated chloroform and DMSO in hydrazonoform. The analgesic and antimicrobial activity of the synthesized compounds was evaluated. Analgesic activity was studied by the "hot plate" thermal irritation method on outbred white mice of both sexes with intraperitoneal injection. Antimicrobial activity of synthesized compounds was established via two-fold serial dilutions method in a liquid growth medium against two strains -S. aureus ATCC 6538-P and E. soli ATCC 25922. The studied compounds showed pronounced analgesic activity significantly exceeding that of the comparison drug metamizole sodium, and in some cases corresponding to the action of the reference diclofenac sodium. Therefore, pronounced analgesic activity accompanied with weak antimicrobial activity of the synthesized hetarylamides determines the prospects for the development of a new pharmacological active substance with an-algesic properties.