| Author/Editor | | Tomašić, Tihomir; Zidar, Nace; Kovač, Andreja; Turk, Samo; Simčič, Mihael; Blanot, Didider; Mueller-Premru, Manica; Filipič, Metka; Golič-Grdadolnik, Simona; Zega, Anamarija; Anderluh, Marko; Gobec, Stanislav; Kikelj, Danijel; Peterlin-Mašič, Lucija |
| Abstract | | Mur ligases participate in the intracellular path of bacterial peptidoglycan biosynthesis and constitute attractive, although so far underexploited, targets for antibacterial drug discovery. A series of hydroxy-substituted 5-benzylidenethiazolidin-4-ones were synthesized and tested as inhibitors of Mur ligases. The most potent compound 5 a was active against MurD-F with IC50 values between 2 and 6 m, making it a promising multitarget inhibitor of Mur ligases. Antibacterial activity against different strains, inhibitory activityagainst protein kinases, mutagenicity and genotoxicity of 5 a were also investigated, and kinetic and NMR studies were conducted.
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