Antidotes to anthrax lethal factor intoxication. Part 3: Evaluation of core structures and further modifications to the C2-side chain.

@article{Jiao2012AntidotesTA,
  title={Antidotes to anthrax lethal factor intoxication. Part 3: Evaluation of core structures and further modifications to the C2-side chain.},
  author={Guan-Sheng Jiao and Seongjin Kim and Mahtab Moayeri and Devorah Crown and April Thai and Lynne Cregar-Hernandez and Linda McKasson and Banumathi Sankaran and Axel T. Lehrer and Teri Ann S. Wong and Lisa Johns and Stephen A. Margosiak and Stephen H Leppla and Alan T. Johnson},
  journal={Bioorganic & medicinal chemistry letters},
  year={2012},
  volume={22 6},
  pages={2242-6}
}
Four core structures capable of providing sub-nanomolar inhibitors of anthrax lethal factor (LF) were evaluated by comparing the potential for toxicity, physicochemical properties, in vitro ADME profiles, and relative efficacy in a rat lethal toxin (LT) model of LF intoxication. Poor efficacy in the rat LT model exhibited by the phenoxyacetic acid series (3) correlated with low rat microsome and plasma stability. Specific molecular interactions contributing to the high affinity of inhibitors… CONTINUE READING