Voltage-gated sodium channel subtype Nav1.7 is a promising drug target associated with neuropathic pain disorder, however, the current Nav1.7 inhibitors show limited efficacy in clinical trials. More new molecular entities need to be discovered. Here, the authors report a selective Nav1.7 inhibitor by using carbenoid-involved reactions to construct an oxindole-based library, applying it to the scaffold-oriented virtual screening, and validating the hit compound in a clinically relevant model.
- Jirong Shu
- Yuwei Wang
- Wenhao Hu
