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  • Title: Synthesis and testing of trifluoromethyl-containing phosphonate-peptide conjugates as inhibitors of serine hydrolases.
    Author: Sokolova NV, Nenajdenko VG, Sokolov VB, Serebryakova OG, Makhaeva GF.
    Journal: Bioorg Med Chem Lett; 2011 Dec 01; 21(23):7216-8. PubMed ID: 22001085.
    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.
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