Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 85, Issue -, Pages 228-234Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.07.095
Keywords
Alzheimer's disease; Amyloid-beta; Tau; Aggregation; Suzuki-Miyaura coupling
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Aggregations of both amyloid-beta (A beta) and hyper-phosphorylated tau proteins are recognized as key pathological manifestations of Alzheimer's disease (AD). Agents that inhibit both those forms of aggregation show promise as drug candidates. Seventeen oligo heteroaromatic compounds were rapidly synthesized via a one-pot, 3- or 4-component coupling procedure. Evaluations showed that compounds E16 and E18 were the most potent inhibitors of A beta and tau aggregations (E16: IC(50)s = 0.38, 0.29 mu M against A beta, tau, respectively, E18: IC(50)s = 0.55, 0.30 mu M against A beta, tau, respectively). (C) 2014 Elsevier Masson SAS. All rights reserved.
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