期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 23, 页码 7216-7218出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.09.030
关键词
Serine hydrolases; Organophosphorous compounds; Inhibitors; Peptides; Click chemistry
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. (C) 2011 Elsevier Ltd. All rights reserved.
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