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Novel 2-thioxothiazolidin-4-one inhibitors of bacterial MurD ligase targeting d-Glu- and diphosphate-binding siteTomašič, Tihomir ...Mur ligases are involved in cytoplasmic steps of bacterial peptidoglycan biosynthesis and are viable targets for antibacterial drug discovery. We have designed and synthesized a focused chemical ... library of compounds combining the glutamic acid moiety and the 2-thioxothiazolidin-4-one, thiazolidine-2,4-dione, 2-iminothiazolidin-4-one or imidazolidine-2,4-dione ring connected by a benzylidene group. These compounds were designed to targetthe d-Glu- and the diphosphate-binding pockets of the MurD active site and were evaluated for inhibition of MurD ligase from Escherichia coli. The most potent compounds (R)-9 and (S)-9 inhibited MurD with IC50 values of 45 [micro]M and 10 [microm]M, respectively. The specific binding mode of (R)-9 in MurD active site was established by high-resolution NMR spectroscopy.Source: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 46, issue 9, 2011, str. 3964-3975)Type of material - article, component partPublish date - 2011Language - englishCOBISS.SI-ID - 3030897
source: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 46, issue 9, 2011, str. 3964-3975)
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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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Tomašič, Tihomir | 28334 |
Kovač, Andreja, farmacevtka, 1979- | 27782 |
Simčič, Mihael | 28554 |
Blanot, Didier | |
Golič Grdadolnik, Simona | 08329 |
Gobec, Stanislav, 1970- | 15284 |
Kikelj, Danijel | 01463 |
Peterlin-Mašič, Lucija | 19317 |
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