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Diethyl 2-(Phenylcarbamoyl)phenyl Phosphorothioates: Synthesis, Antimycobacterial Activity and Cholinesterase Inhibition
Authors: Vinsova Jarmila | Kratky Martin | Komloova Marketa | Dadapeer Echchukattula | Štěpánková Šárka | Vorčáková Katarína | Stolarikova Jirina
Year: 2014
Type of publication: článek v odborném periodiku
Name of source: Molecules
Publisher name: Molecular Diversity Preservation International
Place: Basel
Page from-to: 7152-7168
Titles:
Language Name Abstract Keywords
cze Diethyl 2-(fenylkarbamoyl)fenyl thiofosfáty Celkem 27 nově syntetizovaných diethyl 2(fenylkarbamoyl)fenyl thiofosfátů bylo charakterizováno NMR, IR a CHN a byla hodnocena jejich aktivita vůči Mycobacterium tuberculosis H(37)Rv, Mycobacterium avium a dvěma druhům Mycobacterium kansasii. Nejlepší účinnosti vůči M. tuberculosis bylo dosaženo O-{4-bromo-2-[(3,4-dichlorofenyl)karbamoyl] fenyl} O,O-diethyl thiofosfátem (minimálí inhibiční koncentrace 4 mu M). Nejvyšší účinnost proti netuberkulozní mykobakterii byla prokázána u O-(5-chloro-2-{[4-(trifluoromethyl) fenyl] karbamoyl}fenyl) O, O-diethyl thiofosfátu s MIC od 16 mu M. Připravené thiofosfáty byly také testované na inhibiční účinnost vůči acetylcholinesterase z elektrického úhoře a butyrylcholinesterase z koňského séra. Jejich inhibiční účinnost byla srovnatelná s účinností známých cholinestrasových inhibitorů - galanthaminem a rivastigminem. Všechny testované sloučeniny vykazovaly vyšší (při inhibici AChE) a srovnatelnou (při inhibici BChE) aktivitu jako rivastigmin s hodnotami IC50 v rozmezí 8.04 až 20.2 mu M.
eng Diethyl 2-(Phenylcarbamoyl)phenyl Phosphorothioates: Synthesis, Antimycobacterial Activity and Cholinesterase Inhibition A new series of 27 diethyl 2-(phenylcarbamoyl)phenyl phosphorothioates (thiophosphates) was synthesized, characterized by NMR, IR and CHN analyses and evaluated against Mycobacterium tuberculosis H(37)Rv, Mycobacterium avium and two strains of Mycobacterium kansasii. The best activity against M. tuberculosis was found for O-{4-bromo-2-[(3,4-dichlorophenyl)carbamoyl] phenyl} O,O-diethyl phosphorothioate (minimum inhibitory concentration of 4 mu M). The highest activity against nontuberculous mycobacteria was exhibited by O-(5-chloro-2-{[4-(trifluoromethyl) phenyl] carbamoyl}phenyl) O, O-diethyl phosphorothioate with MIC values from 16 mu M. Prepared thiophosphates were also evaluated against acetylcholinesterase from electric eel and butyrylcholinesterase from equine serum. Their inhibitory activity was compared to that of the known cholinesterases inhibitors galanthamine and rivastigmine. All tested compounds showed a higher (for AChE inhibition) and comparable (for BChE inhibition) activity to that of rivastigmine, with IC(50)s within the 8.04 to 20.2 mu M range. antimycobacterial activity; in vitro acetylcholinesterase inhibition; in vitro butyrylcholinesterase inhibition; salicylanilide; thiophosphates

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