MraY (phospho-N-acetylmuramoyl-pentapeptide-transferase) inhibitory natural products are attractive candidates for the development of agents to combat antimicrobial-resistant bacteria, but their properties need to be improved by structural optimization which is challenging. Here, the authors develop a strategy for a comprehensive in situ evaluation of the build-up library, which enables streamlining of the preparation of the analogue library and direct assessment of its biological activities.
- Kazuki Yamamoto
- Toyotaka Sato
- Satoshi Ichikawa