Design, synthesis, and biological evaluation of Plasmodium falciparum lactate dehydrogenase inhibitors.

@article{Choi2007DesignSA,
  title={Design, synthesis, and biological evaluation of Plasmodium falciparum lactate dehydrogenase inhibitors.},
  author={Seoung-ryoung Choi and Anupam Pradhan and Nicholas L. Hammond and Amar G. Chittiboyina and Babu L. Tekwani and Mitchell A. Avery},
  journal={Journal of medicinal chemistry},
  year={2007},
  volume={50 16},
  pages={3841-50}
}
Plasmodium falciparum lactate dehydrogenase (pfLDH) is a key enzyme for energy generation of malarial parasites and is a potential antimalarial chemotherapeutic target. It is known that the oxamate moiety, a pyruvate analog, alone shows higher inhibition against pfLDH than human LDHs, suggesting that it can be used for the development of selective inhibitors. Oxamic acid derivatives were designed and synthesized. Derivatives 5 and 7 demonstrated activities against pfLDH with IC50 values of 3.13… CONTINUE READING