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inhibitory properties and in vitro protective potency of two new reversible cholinesterase inhibitors with different acetyl/butyrylcholinesterase selectivity
maja vitorović-todorović Military Technical Institute, Belgrade, majavitod@gmail.com sonja bauk Military Technical Institute, Belgrade, bauk.sonja@gmail.com branko drakulić Institute for Chemistry, Technology and Metallurgy, Belgrade, bdrakuli@chem.bg.ac.rs
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Abstract: The inhibitory and protective potency of the two most active compounds belonging to novel class of reversible cholinesterase inhibitors, 4-aryl-4-oxo-N-phenyl-2-aminylbutyramides, are reported. Chosen compounds were tested in vitro for inhibitory activity against Electric Eel acetylcholinesterase and horse serum butyrylcholinesterase, using acetylthiocholine iodide, related to endogenous substrate. Their inhibitory potency expressed as IC50 values and inhibition types were determined. The ability of compounds to protect corresponding enzymes against irreversible inhibition by organophosphates was examined through their influence on the phosphorylation second-order rate constant by diisopropyl fluorophosphate..
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