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Salicylanilide diethyl phosphates as cholinesterases inhibitors
Authors: Kratký Martin | Štěpánková Šárka | Vorčáková Katarína | Vinšová Jarmila
Year: 2015
Type of publication: článek v odborném periodiku
Name of source: Bioorganic Chemistry
Publisher name: Academic Press (Elsevier)
Place: SAN DIEGO
Page from-to: 48-52
Titles:
Language Name Abstract Keywords
cze Diethylfosfáty salicylanilidu jako inhibitory ccholinesteráz U 27 diethylfosfátů salicylanilidu byla hodnocena jejich inhibiční účinnost vůči acetylcholinesteráze z elektrického úhoře a butyrylcholinesteráze z koňského séra. Pro stanovení byla použita Ellmanova metoda. Inhibiční účinnost (vyjádřená jako IC50) byla porovnávána s účinnosti galanthaminu a rivastigminu. Testované salicylanilidy vykazují dobrou inhibiční účinnost vůči oběma cholinesterázám a působí jako pseudo-ireverzibilní inhibitory. Diethylfosfáty salicylanilidu; inhibitory cholinesteráz
eng Salicylanilide diethyl phosphates as cholinesterases inhibitors Based on the presence of dialkyl phosphate moiety, we evaluated twenty-seven salicylanilide diethyl phosphates (diethyl [2-(phenylcarbamoyl) phenyl] phosphates) for the inhibition of acetylcholinesterase (AChE) from electric eel (Electrophorus electricus L.) and butyrylcholinesterase (BChE) from equine serum. Ellman's spectrophotometric method was used. The inhibitory activity (expressed as IC50 values) was compared with that of the established drugs galantamine and rivastigmine. Salicylanilide diethyl phosphates showed significant activity against both cholinesterases with IC50 values from 0.903 to 86.3 mu M. IC(50)s for BChE were comparatively lower than those obtained for AChE. All of the investigated compounds showed higher inhibition of AChE than rivastigmine, and six of them inhibited BChE more effectively than both rivastigmine and galantamine. In general, derivatives of 4-chlorosalicylic acid showed enhanced activity when compared to derivatives of 5-halogenated salicylic acids, especially against BChE. The most effective inhibitor of AChE was O-{5-chloro-2-[(3-bromophenyl) carbamoyl] phenyl} O, O-diethyl phosphate with IC50 of 35.4 mu M, which is also one of the most potent inhibitors of BChE. O-{5-Chloro-2-[( 3,4-dichlorophenyl) carbamoyl] phenyl} O, O-diethyl phosphate exhibited in vitro the strongest inhibition of BChE (0.90 mu M). Salicylanilide diethyl phosphates act as pseudo-irreversible cholinesterases inhibitors. Acetylcholinesterase; Butyrylcholinesterase; Enzyme inhibition; Organophosphate; Salicylanilide diethyl phosphate

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