Design, synthesis and structure–activity relationship (SAR) studies of 2, 4-disubstituted pyrimidine derivatives: Dual activity as cholinesterase and Aβ-aggregation …
A novel class of 2, 4-disubstituted pyrimidines (7a–u, 8a–f, 9a–e) that possess substituents with varying steric and electronic properties at the C-2 and C-4 positions, were designed, synthesized and evaluated as dual cholinesterase and amyloid-β (Aβ)-aggregation inhibitors. In vitro screening identified N-(naphth-1-ylmethyl)-2-(pyrrolidin-1-yl) pyrimidin-4- amine (9a) as the most potent AChE inhibitor (IC50= 5.5 μM). Among this class of ...
