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Investigation of salicylanilide and 4-chlorophenol-based N-monosubstituted carbamates as potential inhibitors of acetyl- and butyrylcholinesterase
Authors: Kratky Martin | Štěpánková Šárka | Vorčáková Katarína | Vinsova Jarmila
Year: 2018
Type of publication: článek v odborném periodiku
Name of source: Bioorganic Chemistry
Publisher name: Elsevier Science Inc.
Place: New York
Page from-to: 668-673
Titles:
Language Name Abstract Keywords
cze Výzkum salicylanilidových a 4-chlorofenol-N-monosubstituovaných karbamátů jako potenciálních inhibitorů acetyl- a butyrylcholinesterázy Ellmanovou metodou byla ověřována inhibiční aktivita salicylanilidových N-monosubstituovaných karbamátů a 4-chlorofenylkarbamátů vůči acetylcholinesteráze z paúhoře elektrického (AChE) a butyrylcholinesteráze (BChE) z koňského séra. Karbamáty a salicylanilidy vykázaly většinou středně silnou inhibici vůči oběma cholinesterázám s hodnotami IC50 v rozmezí 5-235 mikroM. Hodnoty IC50 pro AChE byly v užším rozmezí, než u BChE, ale většina sloučenin vykazovala vyrovnanou inhibici obou cholinesteráz. Při inhibici ACHE byly studované deriváty minimálně stejně účinné nebo účinnější než rivastigmin. Testované sloučeniny také vykazovaly vlastnosti vhodné pro průchod dod CNS. acetylcholinesteráza; butyrylcholinesteráza; karbamáty; inhibice enzymů; salicylanilidy
eng Investigation of salicylanilide and 4-chlorophenol-based N-monosubstituted carbamates as potential inhibitors of acetyl- and butyrylcholinesterase Based on the presence of carbamate moiety, twenty salicylanilide N-monosubstituted carbamates concomitantly with their parent salicylanilides and five newly prepared 4-chlorophenyl carbamates obtained from isocyanates were investigated using Ellman's method for their in vitro inhibitory activity against acetylcholinesterase (AChE) from electric eel and butyrylcholinesterase (BChE) from equine serum. The carbamates and salicylanilides exhibited mostly a moderate inhibition of both cholinesterase enzymes with IC(50) values ranging from 5 to 235 mu M. IC(50) values for AChE were in a narrower concentration range when compared to BChE, but many of the compounds produced a balanced inhibition of both cholinesterases. The derivatives were comparable or superior to rivastigmine for AChE inhibition, but only a few of carbamates also for BChE. Several structure-activity relationships were identified, e.g., N-phenethylcarbamates produce clearly favourable BChE inhibition. The compounds also share convenient physicochemical properties for CNS penetration. Acetylcholinesterase; Butyrylcholinesterase; Carbamate; Enzyme inhibition; Salicylanilide

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