PREPARATION AND ANTIHYPOXIC ACTIVITY OF COMPLEXES OF URACIL DERIVATIVES WITH DICARBOXYLIC ACIDS

摘要

Water-soluble low-toxicity complexes of 6-methyluracil and its derivatives with succinic and fumaric acids were synthesized. The synthesized complexes were tested for antihypoxic activity. Metabolically active drugs that enhance human performance under unfavorable professional ecological conditions have recently been the subject of detailed pharmacological studies. Drugs that produce a positive effect on development mechanisms of the general pathological state such as autoprotectors, antioxidants, antihypoxants, and other metabolic agents are especially interesting. Included in these compounds are pyrimidine derivatives, in particular, 6-methyluracil (6-MU). The majority of pharmacological effects of 6-MU and its derivatives (antidote, hepatoprotector, stress-protector) is known to rely on two primary mechanisms. These are inhibition of free-radical oxidation and direct protective action on biological membranes. However, uracil derivatives have weak effects on energy-generation processes in cells, i.e., they have little antihypoxic activity. It can be enhanced by combined use of the pyrimidines with known antihypoxants, e.g., succinic and fumaric acids. These acids increase both energy generation and stability in an organism under extreme conditions [1].