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- W2007067102 abstract "A series of tetracyclic thienopyrimidines (7–14) was prepared and investigated as inhibitors of acetylcholinesterase from Electrophorus electricus acetylcholinesterase (EeAChE), as well as human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBChE). A new synthetic procedure was employed for the synthesis of the angularly fused heterocycles 7–10. Among them, the presence of a tetrahydropyrido ring with a benzyl rest at the basic nitrogen was required for EeAChE inhibition. A detailed kinetic analysis of the hyperbolic mixed-type inhibition of EeAChE by 9–14 was performed. These heterocyclic compounds inhibited EeAChE with Ki values of less than 3 µM. Most α values were relatively close to 1, indicating a similar affinity of the inhibitor to the free enzyme and the enzyme-substrate complex. Inhibitor 10 displayed a rather uncompetitive pattern of inhibition (α = 0.47) and a relatively high residual activity of a postulated ternary enzyme-substrate-inhibitor complex (β = 0.24)." @default.
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- W2007067102 date "2010-08-31" @default.
- W2007067102 modified "2023-09-27" @default.
- W2007067102 title "Hyperbolic mixed-type inhibition of acetylcholinesterase by tetracyclic thienopyrimidines" @default.
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- W2007067102 doi "https://doi.org/10.3109/14756366.2010.504674" @default.
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