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ID: ALA1921786

Journal: Bioorg Med Chem Lett

Title: Synthesis and testing of trifluoromethyl-containing phosphonate-peptide conjugates as inhibitors of serine hydrolases.

Authors: Sokolova NV, Nenajdenko VG, Sokolov VB, Serebryakova OG, Makhaeva GF.

Abstract: A modification of novel fluorinated organophosphorous compounds containing terminal alkyne group by different azidopeptides via Cu(I)-catalyzed click chemistry has been described. The inhibitor activity of trifluoromethyl-containing methylphosphonates and their peptide-conjugates towards acetylcholinesterase, butyrylcholinesterase, and carboxylesterase has been investigated. It was shown that the incorporation of peptide fragments significantly modulates the esterase profile of starting methylphosphonates.

CiteXplore: 22001085

DOI: 10.1016/j.bmcl.2011.09.030