title: [Non-peptide furin inhibitors based on amidinohydrazones of diarylaldehydes].
abstract: 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.forename: V K
authors.initials: VK
authors.lastname: Kibirev
authors.forename: T V
authors.initials: TV
authors.lastname: Osadchuk
authors.forename: A P
authors.initials: AP
authors.lastname: Kozachenko
authors.forename: O B
authors.initials: OB
authors.lastname: Vadziuk
authors.forename: V S
authors.initials: VS
authors.lastname: Brovarets
mesh_terms: D000447:Aldehydes / Q000138:chemical synthesis*; D003374:Coumarins / Q000737:chemistry; D045683:Furin / Q000037:antagonists & inhibitors* / Q000737:chemistry; D006146:Guanidines / Q000138:chemical synthesis*; D006801:Humans; D006835:Hydrazones / Q000138:chemical synthesis*; D057927:Hydrophobic and Hydrophilic Interactions; D007700:Kinetics; D015394:Molecular Structure; D009842:Oligopeptides / Q000737:chemistry; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors / Q000737:chemistry; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis*; D055672:Static Electricity; D013329:Structure-Activity Relationship
chemical_list: D000447:Aldehydes; D003374:Coumarins; D006146:Guanidines; D006835:Hydrazones; D009842:Oligopeptides; D011994:Recombinant Proteins; D015842:Serine Proteinase Inhibitors; C089959:tert-butoxycarbonyl-arginyl-valyl-arginyl-arginyl-methylcoumarin amide; D045683:Furin