Synthesis and SAR of piperazine amides as novel c-jun N-terminal kinase (JNK) inhibitors

A novel series of c-jun N-terminal kinase (JNK) inhibitors were designed and developed from a high-throughput-screening hit. Through the optimization of the piperazine amide 1, several potent compounds were discovered. The X-ray crystal structure of 4g showed a unique binding mode different from other well known JNK3 inhibitors.

Graphical abstractA novel series of c-jun N-terminal kinase (JNK) inhibitors were designed and developed from high-throughput-screening lead 1.Figure optionsDownload full-size imageDownload as PowerPoint slide