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Salicylanilide diethyl phosphates as potential inhibitors of some mycobacterial enzymes.

ABSTRACT: 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 ?-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 µM 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.

SUBMITTER: Kratky M

PROVIDER: S-EPMC4236894 | biostudies-literature | 2014

REPOSITORIES: biostudies-literature

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Salicylanilide diethyl phosphates as potential inhibitors of some mycobacterial enzymes.

Krátký Martin M Novotná Eva E Saxena Shalini S Yogeeswari Perumal P Sriram Dharmarajan D Švarcová Markéta M Vinšová Jarmila J

TheScientificWorldJournal 20141104

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 ε-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 agai ...[more]

PMID: 25538961

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