NON-PEPTIDE FURIN INHIBITORS BASED ON AMIDINOHYDRAZONES OF DIARYLALDEHYDES
V. K. Kibirev1, T. V. Osadchuk2, O. P. Kozachenko2, O. B. Vadzyuk1, V. S. Brovarets2
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.
Key words: furin, diamidinohydrazones of dialdehydes, furin inhibitors.
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