Prevention of the formation of advanced glycation end-products (AGEs) is a reliable approach to achieve control over hyperglycemia and the associated pathogenesis of diabetic vascular complications. In these terms, new synthetic approaches to 6-nitroazolo[1,5-a]pyrimidines have been developed on the basis of the promising antiglycation activity of their structural analogues, such as azolo[5,1-c][1,2,4]triazine-4(1H)-ones. A number of nitroazolopyrimidines were obtained by using nitration, chlorodeoxygenation, and amination reactions, and their antidiabetic properties were elucidated in vitro. It was shown that triazolo[1,5-a]pyrimidine-7(4H)-ones exhibit a higher antiglycation activity than the corresponding 7-alkylamino analogs and aminoguanidine, as the reference compound. It is suggested that this kind of activity can be associated with the chelating properties possessed by the synthesized 6-nitro-7-oxoderivatives. Furthermore, the compounds obtained were tested for their inhibitory activity against dipeptidyl peptidase 4 (DPP4), glycogen phosphorylase, and α-glucosidase in vitro, but their activities proved to be significantly inferior to those of the reference compounds.
В данном исследовании описана оптимизация методики медь-индуцированного аутоокисления аскорбиновой кислоты как способа оценки хелатирующей активности веществ на примере пиоглитазона. В процесс регистрации данных была внедрена техника real-time. Анализ данных проведен с применением интегральных исчислений и последующей кластеризацией данных. Это позволило вести более быстрое определение активности и использовать в сравнительном анализе одну концентрацию в противовес стандартному концентрационному исследованию.Ключевые слова: аскорбиновая кислота, многофункциональная антиоксидантность, хелация, сульфат меди (II), исследование в реальном времени.
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