Synthesis, Molecular Docking, and Hemorheological Activity of New 4-(Thien-2-yl)-3-aminopyridine-2(1H)-one Derivatives
Palamarchuk I.V. Shulgau Z.T. Sergazy S.D. Zhulikeeva A.M. Seilkhanov T.M. Kulakov I.V.
September 2022Pleiades journals
Russian Journal of General Chemistry
2022#92Issue 91692 - 1705 pp.
Abstract: On the basis of 4-(thien-2-yl)-3-aminopyridine-2(1H)-one, the corresponding chloroacetamide and condensed 1H-pyrido[2,3-b][1,4]oxazine-2(3H)-one were synthesized by the reaction of acylation with chloroacetyl chloride. Thioureide derivatives of 3-aminopyridine-2(1H)-one were obtained by reactions with a number of isothiocyanates. It was shown that the carbamothionylmethacrylamide derivative cyclizes rather easily into substituted 1,3-thiazine. Molecular docking of synthesized derivatives for antithrombotic activity was carried out, which showed that the presence of a thiourea fragment in the pyridone core leads to an increase in affinity for the selected protein. The hemorheological study of the compounds using the in vitro model of the increased blood viscosity syndrome also showed activity at the level of the reference drug pentoxifylline.
1H-pyrido[2,3-b][1,4]oxazin-2(3H)-one , 3-aminopyridine-2(1H)-one , hemorheological activity , intramolecular heterocyclization , thiophene derivatives , thioureide derivatives
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Tyumen State University, Tyumen, 625003, Russian Federation
Republican State Enterprise “National Center for Biotechnology”, Nur-Sultan, 010000, Kazakhstan
Sh. Ualikhanov Kokshetau State University, Kokshetau, 020000, Kazakhstan
Tyumen State University
Republican State Enterprise “National Center for Biotechnology”
Sh. Ualikhanov Kokshetau State University
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