About: Diethyl 2-(Phenylcarbamoyl)phenyl Phosphorothioates: Synthesis, Antimycobacterial Activity and Cholinesterase Inhibition

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About: Diethyl 2-(Phenylcarbamoyl)phenyl Phosphorothioates: Synthesis, Antimycobacterial Activity and Cholinesterase Inhibition Goto Sponge NotDistinct Permalink

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
rdfs:seeAlso	http://www.mdpi.com/1420-3049/19/6/7152/htm
Description	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. 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. (en)
Title	Diethyl 2-(Phenylcarbamoyl)phenyl Phosphorothioates: Synthesis, Antimycobacterial Activity and Cholinesterase Inhibition Diethyl 2-(Phenylcarbamoyl)phenyl Phosphorothioates: Synthesis, Antimycobacterial Activity and Cholinesterase Inhibition (en)
skos:prefLabel	Diethyl 2-(Phenylcarbamoyl)phenyl Phosphorothioates: Synthesis, Antimycobacterial Activity and Cholinesterase Inhibition Diethyl 2-(Phenylcarbamoyl)phenyl Phosphorothioates: Synthesis, Antimycobacterial Activity and Cholinesterase Inhibition (en)
skos:notation	RIV/00216208:11160/14:10281975!RIV15-MSM-11160___
http://linked.open...avai/riv/aktivita	I P S
http://linked.open...avai/riv/aktivity	I, P(EE2.3.20.0235), P(EE2.3.30.0022), P(EE2.3.30.0061), S
http://linked.open...iv/cisloPeriodika	6
http://linked.open...vai/riv/dodaniDat	2015
http://linked.open...aciTvurceVysledku	Krátký, Martin Vinšová, Jarmila Komlóová, Markéta Echchukattula, Dadapeer
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Univerzita Karlova v Praze / Farmaceutická fakulta v Hradci Králové
http://linked.open...dnocenehoVysledku	11401
http://linked.open...ai/riv/idVysledku	RIV/00216208:11160/14:10281975
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	thiophosphates; salicylanilide; in vitro butyrylcholinesterase inhibition; in vitro acetylcholinesterase inhibition; antimycobacterial activity (en)
http://linked.open.../riv/klicoveSlovo	thiophosphates salicylanilide in vitro acetylcholinesterase inhibition in vitro butyrylcholinesterase inhibition antimycobacterial activity
http://linked.open...odStatuVydavatele	CH - Švýcarská konfederace
http://linked.open...ontrolniKodProRIV	[8A43B4D6A7A7]
http://linked.open...i/riv/nazevZdroje	Molecules
http://linked.open...in/vavai/riv/obor	FR
http://linked.open...ichTvurcuVysledku	4 (xsd:int)
http://linked.open...cetTvurcuVysledku	7 (xsd:int)
http://linked.open...vavai/riv/projekt	Increasing of the R&D capacity at Charles University through new positions for graduates of doctoral studies Establishment of Research Team Focused on Experimental and Applied Biopharmacy Support of establishment, development, and mobility of quality research teams at the Charles University
http://linked.open...UplatneniVysledku	2014
http://linked.open...v/svazekPeriodika	19
http://linked.open...iv/tvurceVysledku	Krátký, Martin Vinšová, Jarmila Stolaříková, Jiřina Komlóová, Markéta Štěpánková, Šárka Vorčáková, Katarína Echchukattula, Dadapeer
http://linked.open...ain/vavai/riv/wos	000338586700015
issn	1420-3049
number of pages	17 (xsd:int)
http://bibframe.org/vocab/doi	10.3390/molecules19067152
http://localhost/t...ganizacniJednotka	11160

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