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  • Title: 6-Nitroazolo[1,5-a]pyrimidin-7(4H)-ones as Antidiabetic Agents.
    Author: Spasov AA, Babkov DA, Sysoeva VA, Litvinov RA, Shamshina DD, Ulomsky EN, Savateev KV, Fedotov VV, Slepukhin PA, Chupakhin ON, Charushin VN, Rusinov VL.
    Journal: Arch Pharm (Weinheim); 2017 Dec; 350(12):. PubMed ID: 29152780.
    Abstract:
    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.
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