Discovery of Novel 5-Benzylidenerhodanine and 5-Benzylidenethiazolidine-2,4-dione Inhibitors of MurD Ligase
Journal of Medicinal Chemistry2010Vol. 53(18), pp. 6584–6594
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Nace Zidar, Tihomir Tomašič, Roman Šink, Veronika Rupnik, Andreja Kovač, Samo Turk, Delphine Patin, Didier Blanot, Carlos Contreras Martel, Andréa Dessen, Manica Müller Premru, Anamarija Zega, Stanislav Gobec, Lucíja Peterlin Mašič, D. Kikelj
Abstract
We have designed, synthesized, and evaluated 5-benzylidenerhodanine- and 5-benzylidenethiazolidine-2,4-dione-based compounds as inhibitors of bacterial enzyme MurD with E. coli IC(50) in the range 45-206 μM. The high-resolution crystal structure of MurD in complex with (R,Z)-2-(3-[{4-([2,4-dioxothiazolidin-5-ylidene]methyl)phenylamino}methyl)benzamido)pentanedioic acid [(R)-32] revealed details of the binding mode of the inhibitor within the active site and provides a good foundation for structure-based design of a novel generation of MurD inhibitors.
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