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ID: ALA1155211

Journal: Bioorg Med Chem Lett

Title: Synthesis of organophosphates with fluorine-containing leaving groups as serine esterase inhibitors with potential for Alzheimer disease therapeutics.

Authors: Makhaeva GF, Aksinenko AY, Sokolov VB, Serebryakova OG, Richardson RJ.

Abstract: Acetylcholinesterase and butyrylcholinesterase inhibitors are potential cognition enhancers in Alzheimer disease. O,O-Dialkylphosphate inhibitors with 1-substituted 2,2,2-trifluoroethoxy leaving groups were synthesized by phosphonate-phosphate rearrangement. Substituents in the 1-position of the leaving group along with the O-alkyl groups modulated potency and selectivity against acetylcholinesterase, butyrylcholinesterase, and carboxylesterase.

CiteXplore: 19717305

DOI: 10.1016/j.bmcl.2009.08.065