Triazaspirodimethoxybenzoyls as selective inhibitors of mycobacterial lipoamide dehydrogenase .

@article{Bryk2010TriazaspirodimethoxybenzoylsAS,
  title={Triazaspirodimethoxybenzoyls as selective inhibitors of mycobacterial lipoamide dehydrogenase .},
  author={Ruslana Bryk and Nancy M Arango and Aditya Venugopal and J David Warren and Yun-hee Park and Mulchand S. Patel and Christopher D Lima and Carl Nathan},
  journal={Biochemistry},
  year={2010},
  volume={49 8},
  pages={1616-27}
}
Mycobacterium tuberculosis (Mtb) remains the leading single cause of death from bacterial infection. Here we explored the possibility of species-selective inhibition of lipoamide dehydrogenase (Lpd), an enzyme central to Mtb's intermediary metabolism and antioxidant defense. High-throughput screening of combinatorial chemical libraries identified triazaspirodimethoxybenzoyls as high-nanomolar inhibitors of Mtb's Lpd that were noncompetitive versus NADH, NAD(+), and lipoamide and >100-fold… CONTINUE READING