Synthesis and structure-activity relationships of truncated bisubstrate inhibitors of aminoglycoside 6'-N-acetyltransferases.

@article{Gao2006SynthesisAS,
  title={Synthesis and structure-activity relationships of truncated bisubstrate inhibitors of aminoglycoside 6'-N-acetyltransferases.},
  author={Feng Gao and Xuxu Yan and Tushar Shakya and Oliver M. Baettig and Samia Ait-Mohand-Brunet and Albert M Berghuis and Gerard D. Wright and Karine Auclair},
  journal={Journal of medicinal chemistry},
  year={2006},
  volume={49 17},
  pages={5273-81}
}
Truncated aminoglycoside-coenzyme A bisubstrate analogues were efficiently prepared using a convergent approach where the amine and the thiol are coupled in one pot with the addition of a linker, without the need for protecting groups. These derivatives were tested for their effect on the activity of the resistance-causing enzyme aminoglycoside 6'-N… CONTINUE READING