1224734-27-3Relevant articles and documents
Design, synthesis and biological evaluation of indane-2-arylhydrazinylmethylene-1,3-diones and indol-2-aryldiazenylmethylene-3-ones as β-amyloid aggregation inhibitors
Catto, Marco,Aliano, Rosaria,Carotti, Angelo,Cellamare, Saverio,Palluotto, Fausta,Purgatorio, Rosa,De Stradis, Angelo,Campagna, Francesco
experimental part, p. 1359 - 1366 (2010/06/14)
Biological screening of (hetero)aromatic compounds allowed the identification of some novel inhibitors of Aβ1-40 aggregation, bearing indane and indole rings as common scaffolds. Molecular decoration of lead compounds led to inhibitors exhibiting a potency, measured by the Thioflavin T fluorimetric assay, ranging from high to low micromolar IC50. The 2-(p-isopropylphenyldiazenylmethylene)indolone derivative 6c resulted as the most potent aggregation inhibitor exhibiting an IC50 of 1.4?μM, with complete lack of fibril formation as confirmed by transmission electron microscopy. Structure-activity relationships suggested that binding to the Aβ peptide may be largely guided by π-stacking and hydrogen bond interactions.