LpxC Inhibitor

Researchers from industry and academia have synthesized structurally diverse LpxC inhibitors, exhibiting different LpxC inhibitory and antibacterial activities. Current search for novel LpxC inhibitors is focused on small molecules, sharing common structural features like a Zn2+-chelating group as well as a highly lipophilic side-chain. However, despite the promising preclinical data of many of the reported compounds, no other LpxC inhibitor, besides the recently withdrawn clinical candidate ACHN-975, has entered clinical trials. The lack of clinical candidates might be related with undesired effects caused by the common structural elements of the LpxC inhibitors. Among the disclosed compounds, the N-aroyl-L-threonine- and methylsulfone-based LpxC inhibitors represent the most promising classes with respect to LpxC inhibitory and antibacterial activities.

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