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Papers of the Week

Papers: 29 Apr 2023 - 5 May 2023

Basic Science

In Vitro Studies, Molecular/Cellular, Pharmacology/Drug Development

2023 Apr 20

Bioorg Med Chem



Design, synthesis, and biological evaluation of acyl sulfonamide derivatives with spiro cycles as Na1.7 inhibitors for antinociception.


Ouyang X, Su M, Xue D, Dong L, Niu H, Li W, Liu Y, Wang K, Shao L


Chronic pain, as an unmet medical need, severely impacts the quality of life. The voltage-gated sodium channel Na1.7 preferentially expressed in sensory neurons of dorsal root ganglia (DRG) serves a promising target for pain therapy. Here, we report the design, synthesis, and evaluation of a series of acyl sulfonamide derivatives targeting Nav1.7 for their antinociceptive activities. Among the derivatives tested, the compound 36c was identified as a selective and potent Na1.7 inhibitor in vitro and exhibited antinociceptive effects in vivo. The identification of 36c not only provides a new insight into the discovery of selective Na1.7 inhibitors, but also may hold premise for pain therapy.