About: Salicylanilide Diethyl Phosphates as Potential Inhibitors of Some Mycobacterial Enzymes     Goto   Sponge   NotDistinct   Permalink

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Description
  • Antimycobacterially active salicylanilide diethyl phosphates were evaluated to identify their potential drug target(s) for the inhibition of several mycobacterial enzymes, including isocitrate lyase, L-alanine dehydrogenase (MtAlaDH), lysine epsilon-aminotransferase, chorismate mutase, and pantothenate synthetase. The enzymes are related to the nongrowing state of Mycobacterium tuberculosis. Salicylanilide diethyl phosphates represent new candidates with significant inhibitory activity especially against L-alanine dehydrogenase. The most active MtAlaDH inhibitor, 5-chloro-2-[(3-chlorophenyl)carbamoyl]phenyl diethyl phosphate, has an IC50 of 4.96 mu M and the best docking results. Other mycobacterial enzymes were mostly inhibited by some derivatives but at higher concentrations; isocitrate lyase showed the highest resistance to salicylanilide diethyl phosphates.
  • Antimycobacterially active salicylanilide diethyl phosphates were evaluated to identify their potential drug target(s) for the inhibition of several mycobacterial enzymes, including isocitrate lyase, L-alanine dehydrogenase (MtAlaDH), lysine epsilon-aminotransferase, chorismate mutase, and pantothenate synthetase. The enzymes are related to the nongrowing state of Mycobacterium tuberculosis. Salicylanilide diethyl phosphates represent new candidates with significant inhibitory activity especially against L-alanine dehydrogenase. The most active MtAlaDH inhibitor, 5-chloro-2-[(3-chlorophenyl)carbamoyl]phenyl diethyl phosphate, has an IC50 of 4.96 mu M and the best docking results. Other mycobacterial enzymes were mostly inhibited by some derivatives but at higher concentrations; isocitrate lyase showed the highest resistance to salicylanilide diethyl phosphates. (en)
Title
  • Salicylanilide Diethyl Phosphates as Potential Inhibitors of Some Mycobacterial Enzymes
  • Salicylanilide Diethyl Phosphates as Potential Inhibitors of Some Mycobacterial Enzymes (en)
skos:prefLabel
  • Salicylanilide Diethyl Phosphates as Potential Inhibitors of Some Mycobacterial Enzymes
  • Salicylanilide Diethyl Phosphates as Potential Inhibitors of Some Mycobacterial Enzymes (en)
skos:notation
  • RIV/00216208:11160/14:10281951!RIV15-MSM-11160___
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • I, P(EE2.3.20.0235), P(EE2.3.30.0022)
http://linked.open...iv/cisloPeriodika
  • November
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
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  • 43724
http://linked.open...ai/riv/idVysledku
  • RIV/00216208:11160/14:10281951
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • pantothenate synthetase; chorismate mutase; lysine epsilon-aminotransferase; L-alanine dehydrogenase; isocitrate lyase; Mycobacterial enzyme; salicylanilide diethyl phosphates (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • US - Spojené státy americké
http://linked.open...ontrolniKodProRIV
  • [62A0DE565A2C]
http://linked.open...i/riv/nazevZdroje
  • The Scientific World Journal
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http://linked.open...ichTvurcuVysledku
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http://linked.open...vavai/riv/projekt
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 2014
http://linked.open...iv/tvurceVysledku
  • Krátký, Martin
  • Novotná, Eva
  • Vinšová, Jarmila
  • Švarcová, Markéta
  • Dharmarajan, Sriram
  • Perumal, Yogeeswari
  • Shalini, Saxena
issn
  • 1537-744X
number of pages
http://bibframe.org/vocab/doi
  • 10.1155/2014/703053
http://localhost/t...ganizacniJednotka
  • 11160
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