In silico consensus activity prediction, rational synthesis, and evaluation of antiglycation and antiplatelet activities of 3,6-disubstituted 1,2,4,5-tetrazines

According to the in silico consensus activity prediction, a series of 3,6-disubstituted 1,2,4,5-tetrazines were synthesized as promising inhibitors of the Maillard reaction. In addition to the studies of antiglycation activity, a comparative in vitro evaluation of the effect of the synthesized compo...

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Veröffentlicht in:Russian chemical bulletin 2020-04, Vol.69 (4), p.768-773
Hauptverfasser: Ishmetova, R. I., Babkov, D. A., Kucheryavenko, A. F., Babkova, V. A., Sirotenko, V. S., Ignatenko, N. K., Tolschina, S. G., Vassiliev, P. M., Rusinov, G. L., Spasov, A. A.
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Sprache:eng
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Zusammenfassung:According to the in silico consensus activity prediction, a series of 3,6-disubstituted 1,2,4,5-tetrazines were synthesized as promising inhibitors of the Maillard reaction. In addition to the studies of antiglycation activity, a comparative in vitro evaluation of the effect of the synthesized compounds on the ADP-induced rabbit platelet aggregation model was carried out. Compounds with antiglycation and antiplatelet activities significantly higher than that of the reference drugs, aminoguanidine and acetylsalicylic acid, were revealed.
ISSN:1066-5285
1573-9171
DOI:10.1007/s11172-020-2831-6