As a result of in vitro screening studies to search for the possible antidiabetic activity of a number of azoloazine derivatives, it was found that the compounds are capable of moderate inhibition of dipeptidylpeptidase-4 (DPP-4), inhibiting the enzyme activity by an average of 60 % at a concentration of 100 цМ, which is inferior actions of the reference drug vildagliptin (more than 99 % of the suppression of the activity of DPP-4 at the same concentration). The compounds are also able to significantly slow down glycation of bovine serum albumin (BSA) (the series leader - compound 1c suppresses the glycation reaction of BSA by 74 % at a concentration of 1 mM, compared to 58 % inhibition for the reference compound aminoguanidine). It was not possible to establish the ability of compounds to bind (chelate) Cu2+ in the ascorbic acid autooxidation test, except for compound 1k (it slowed down the reaction by 49 % at a concentration of 40 цМ, which is comparable in activity to the reference drug pioglitazone and is slightly more active than lipoic acid). The restriction for establishing the copper-binding activity of other members of the series is due to the high light absorption at the working wavelength of 265 nm and is not a criterion for excluding chelating properties. The results allow us to conclude that the class of compounds is a promising basis for the further development of tools with anti-glycating activity based on the structures of the representatives of the series.