Journal of VolgSMU
Quarterly scientific-practical journal

UDK: 615.017:616.079


E.V. Sokolova1, E.A. Hohlacheva1, D.D. SHamshina1, A.E. Batychyok1, P.A. Radaev1, N.A. Prokof eva1, R.A. Litvinov1, D.A. Babkov1, K.V. Savateev2, V.V. Fedotov2

1ФГБОУ ВО «Волгоградский государственный медицинский университет» Министерства здравоохранения Российской Федерации; 2ФГАОУ ВО «УрФУ имени первого Президента России Б.Н. Ельцина»


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 μM, 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 μM, 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.


azoloazine, glycation, DPP-4, chelation, copper.


Литвинов Роман Александрович – к. м. н., ассистент кафедры фармакологии и биоинформатики, e-mail: