Archive des Bibliothèques universitaires de Nantes

Synthèse et évaluation pharmacologique de 36 diaryl 25 dihydroxy 14 benzoquinones à activité insulinomimétique ; Texte imprimé / Alexandra Dassonville ; sous la dir de Guillaume Le Baut

Par : Dassonville , Alexandra -- 1976

Document archivé le : 10/03/2010

Demethylasterriquinone B1 is a nonpeptidyl, small natural molecule, recently discovered, by screening, as an insulin mimetic agent. In this way, we have developped a synthetic method for the preparation of 3,6-diaryl-2,5-dihydroxy-1,4-benzoquinones, analogues of this compounds. The access to these benzoquinones may be envisaged from 3-aryl-1-hydroxypropan-2-ones via 4-aryl-6-arylméthylidène-3-hydroxypyrane-2,5-diones, products of condensation of 4-aryl-3-hydroxypyrane-2,5-diones and aromatic aldehydes. So, several methods for the synthesis of ketol and aldehyde intermediates were investigated in details in this work. The target benzoquinones were evaluated in vitro, on insulin receptor and protein kinase B phophorylation, a key molecule in the transduction signal of insulin. The most active structures were orally administrated to hyperglycemic and hyperinsulinemic mice. The first pharmacological results confirm the interest of such compounds as insulin mimetic agents. 2003NANT02VS

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