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Phosphorylated hydroxyethylamines as novel inhibitors of the bacterial cell wall biosynthesis enzymes MurC to MurFSova, Matej, 1979- ...Enzymes involved in the biosynthesis of bacterial peptidoglycan represent important targets for development of new antibacterial drugs. Among them, Mur ligases (MurC to MurF) catalyze the formation ... of the final cytoplasmic precursor UDP-N-acetylmuramyl-pentapeptide from UDP-N-acetylmuramic acid. We present the design, synthesis and biological evaluation of a series of phosphorylated hydroxyethylamines as new type of small-molecule inhibitors of Mur ligases. We show that the phosphate group attached to the hydroxyl moiety of the hydroxyethylamine core is essential for good inhibitory activity. The IC50 values of these inhibitors were in the micromolar range, which makes thema promising starting point for the development of multiple inhibitors of Mur ligases as potential antibacterial agents. In addition, 1-(4-methoxyphenylsulfonamido)-3-morpholinopropan-2-yl dihydrogen phosphate 7awas discovered as one of the best inhibitors of MurE described so far.Source: Bioorganic chemistry. - ISSN 0045-2068 (Issue 6, Vol. 37, 2009, str. 217-222)Type of material - article, component partPublish date - 2009Language - englishCOBISS.SI-ID - 2637169
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Sova, Matej, 1979- | 25490 |
Kovač, Andreja, farmacevtka, 1979- | 27782 |
Turk, Samo | 29773 |
Hrast, Martina | 32036 |
Blanot, Didier | |
Gobec, Stanislav, 1970- | 15284 |
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