New antidiabetic agents are being sought because of the global problem with diabetes. Amidoxime derivatives are known to have antidiabetic activity. β-Aminopropionamidoxime bases and pharmacologically acceptable salts of O-aroyl-β-(morpholin-1-yl)propionamidoximes and 5-substituted phenyl-3-β-(piperidin-1-yl and morpholin-1-yl)ethyl-1,2,4-oxadiazoles were screened in vitro for antidiabetic activity manifested as inhibition of α-amylase and α-glucosidase. Compounds with pronounced antidiabetic properties were identified. The series of 3,5-disubstituted 1,2,4-oxadiazoles were more active than the series of O-aroyl-β-aminopropionamidoximes. The results could be used for further in vivo screening of the antidiabetic properties of the most promising compounds with a preliminary assessment of their mean toxic doses in animals.
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 53, No. 2, pp. 37 – 41, February, 2019.
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Kayukova, L.A., Uzakova, A.B., Baitursynova, G.P. et al. Inhibition of α-Amylase and α-Glucosidase by New β-Aminopropionamidoxime Derivatives. Pharm Chem J 53, 129–133 (2019). https://doi.org/10.1007/s11094-019-01966-5
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DOI: https://doi.org/10.1007/s11094-019-01966-5