title: Synthesis and testing of trifluoromethyl-containing phosphonate-peptide conjugates as inhibitors of serine hydrolases.
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.
authors: Department of Chemistry, Moscow State University, Moscow, Russia.
authors: Nadezhda V
authors: NV
authors: Sokolova
authors: Valentine G
authors: VG
authors: Nenajdenko
authors: Vladimir B
authors: VB
authors: Sokolov
authors: Olga G
authors: OG
authors: Serebryakova
authors: Galina F
authors: GF
authors: Makhaeva
mesh_terms: D043182:Carboxylesterase / Q000037:antagonists & inhibitors; D002384:Catalysis; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D057930:Click Chemistry; D004789:Enzyme Activation / Q000187:drug effects; D005461:Fluorine / Q000737:chemistry; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D063065:Organophosphonates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D010455:Peptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D002800:Cholinesterase Inhibitors; D063065:Organophosphonates; D010455:Peptides; D015842:Serine Proteinase Inhibitors; D005461:Fluorine; D043182:Carboxylesterase