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Pubmed ID :23534287
Publication Date : 2013/03/28

[Non-peptide furin inhibitors based on amidinohydrazones of diarylaldehydes].


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 microM.

Authors : Kibirev V K , Osadchuk T V , Kozachenko A P , Vadziuk O B , Brovarets V S ,

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