| Autor: |
Vladimir L, Rusinov, Irina M, Sapozhnikova, Anastasiya M, Bliznik, Oleg N, Chupakhin, Valery N, Charushin, Alexander A, Spasov, Pavel M, Vassiliev, Valentina A, Kuznetsova, Andrey I, Rashchenko, Denis A, Babkov |
| Rok vydání: |
2016 |
| Předmět: |
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| Zdroj: |
Archiv der Pharmazie. 350(5) |
| ISSN: |
1521-4184 |
| Popis: |
Inhibition of the dipeptidyl peptidase-4 (DPP4) enzyme activity and prevention of advanced glycation end (AGE) products formation represents a reliable approach to achieve control over hyperglycemia and the associated pathogenesis of diabetic vascular complications. In the frames of this research study, several triazolo- and pyrazolotriazines were synthesized and evaluated as inhibitors of AGE products formation, DPP4, glycogen phosphorylase and α-glucosidase activities, as well as AGE cross-link breakers. From the two considered classes of heterocyclic compounds, the pyrazolotriazines showed the highest potency as antiglycating agents and DPP4 inhibitors. Structure-activity relationships (SAR) for these compounds, which can be considered as potential drugs for the treatment of type 2 diabetes, were evaluated. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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