Ukr.Biochem.J. 2013; Volume 85, Issue 1, Jan-Feb, pp. 22-32


Non-peptide furin inhibitors based on amidinohydrazones of diarylaldehydes

V. K. Kibirev1, T. V. Osadchuk2, O. P. Kozachenko2,
O. B. Vadzyuk1, V. S. Brovarets2

1Palladin Institute of Biochemistry, National Academy of Sciences of Ukraine, Kyiv;
2Institute of Bioorganic Chemistry and Petrochemistry, National Academy of Sciences of Ukraine, Kyiv

A series of novel non-peptidic furin inhibitors containing amidinohydrazone moieties has been synthesized under interaction of dialdehydes, the derivatives of ethylene diethylvanillin ethers, with aminoguanidine bicarbonate. Two aryl cycles were bridged by 1,2-ethylene-, 1,4-buthylene- or 1,4-dimethylenebenzene-group. The compounds have been found to inhibit furin. The antifurin activity was shown to grow with the increase of the length and/or hydrophobicity of the bridge. The most potent compound, containing in the bridge the lypophylic benzene cycle was found to inhibit the activity of furin with Ki = 0.51 µM.

Keywords: , ,


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