Salicylanilide Diethyl Phosphates as Potential Inhibitors of Some Mycobacterial Enzymes
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 sy...
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| Format: | Article |
| Language: | English |
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Wiley
2014-01-01
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| Series: | The Scientific World Journal |
| Online Access: | http://dx.doi.org/10.1155/2014/703053 |
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| author | Martin Krátký Eva Novotná Shalini Saxena Perumal Yogeeswari Dharmarajan Sriram Markéta Švarcová Jarmila Vinšová |
| author_facet | Martin Krátký Eva Novotná Shalini Saxena Perumal Yogeeswari Dharmarajan Sriram Markéta Švarcová Jarmila Vinšová |
| author_sort | Martin Krátký |
| collection | DOAJ |
| 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 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 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. |
| format | Article |
| id | doaj-art-f2c3bffefd34459b81c1415846b21052 |
| institution | Kabale University |
| issn | 2356-6140 1537-744X |
| language | English |
| publishDate | 2014-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | The Scientific World Journal |
| spelling | doaj-art-f2c3bffefd34459b81c1415846b210522025-02-03T07:24:06ZengWileyThe Scientific World Journal2356-61401537-744X2014-01-01201410.1155/2014/703053703053Salicylanilide Diethyl Phosphates as Potential Inhibitors of Some Mycobacterial EnzymesMartin Krátký0Eva Novotná1Shalini Saxena2Perumal Yogeeswari3Dharmarajan Sriram4Markéta Švarcová5Jarmila Vinšová6Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University in Prague, Heyrovského 1203, 500 05 Hradec Králové, Czech RepublicDepartment of Biochemical Sciences, Faculty of Pharmacy, Charles University in Prague, Heyrovského 1203, 500 05 Hradec Králové, Czech RepublicMedicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Hyderabad 500078, IndiaMedicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Hyderabad 500078, IndiaMedicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Hyderabad 500078, IndiaDepartment of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University in Prague, Heyrovského 1203, 500 05 Hradec Králové, Czech RepublicDepartment of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University in Prague, Heyrovského 1203, 500 05 Hradec Králové, Czech RepublicAntimycobacterially 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 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.http://dx.doi.org/10.1155/2014/703053 |
| spellingShingle | Martin Krátký Eva Novotná Shalini Saxena Perumal Yogeeswari Dharmarajan Sriram Markéta Švarcová Jarmila Vinšová Salicylanilide Diethyl Phosphates as Potential Inhibitors of Some Mycobacterial Enzymes The Scientific World Journal |
| title | Salicylanilide Diethyl Phosphates as Potential Inhibitors of Some Mycobacterial Enzymes |
| title_full | Salicylanilide Diethyl Phosphates as Potential Inhibitors of Some Mycobacterial Enzymes |
| title_fullStr | Salicylanilide Diethyl Phosphates as Potential Inhibitors of Some Mycobacterial Enzymes |
| title_full_unstemmed | Salicylanilide Diethyl Phosphates as Potential Inhibitors of Some Mycobacterial Enzymes |
| title_short | Salicylanilide Diethyl Phosphates as Potential Inhibitors of Some Mycobacterial Enzymes |
| title_sort | salicylanilide diethyl phosphates as potential inhibitors of some mycobacterial enzymes |
| url | http://dx.doi.org/10.1155/2014/703053 |
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