Синтез и строение пиридиноилгидразонов димефосфона, обладающих антими-кобактериальной активностью

Nicotinoylhydrazone and isonicotinoylhydrazone of 2-dimethoxyphosphoryl-2-methylpentan-4-one (active component of drug Dimephosphone) have been synthesized. It is established that the crystals of both hydrazones contain a single spatial form of E C =N isomer. In solutions o low-polarity and polar solvents, both dimephosphone pyridinoylhydrazones exist in the form of two amide conformers of the same E C =N isomer. This is related to retarded internal rotation of the molecular fragments around amide bond (O=)C–N. The ratio of conformers is determined by the nature of solvent and the time of solution preparation. Both hydrazones possess low toxicity and high antimycobacterial activity.