Discovery of novel 5-benzylidenerhodanine and 5-benzylidenethiazolidine-2,4-dione inhibitors of MurD ligase.

@article{Zidar2010DiscoveryON,
  title={Discovery of novel 5-benzylidenerhodanine and 5-benzylidenethiazolidine-2,4-dione inhibitors of MurD ligase.},
  author={Nace Zidar and Tihomir Toma{\vs}i{\vc} and R. Kehl Sink and Veronika Rupnik and Andreja Bujan Kovac and Samo Turk and Delphine Patin and Didier Blanot and Carlos Contreras Martel and Andr{\'e}a Dessen and Manica Mueller Premru and Anamarija Zega and Stanislav Gobec and Luc{\'i}ja Peterlin Ma{\vs}i{\vc} and Danijel Kikelj},
  journal={Journal of medicinal chemistry},
  year={2010},
  volume={53 18},
  pages={6584-94}
}
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… CONTINUE READING

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