Abstract
AbstractA chemoselective approach is reported for the synthesis of 4‐(bromo/chloro)methyl‐2‐methylsulfanyl‐6‐trihalomethyl pyrimidines and subsequent nucleophilic substitution of the halomethyl moiety with aminoalcohols. The final compounds were choline derivatives (bearing a pyrimidine ring). These were tested as AChE and BChE inhibitors, and presented IC50 values in the range of 13.8–81.6 μM. Remarkably, the trichloromethyl pyrimidines were the most active compounds. Docking studies and ADMET properties are also reported.
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