The Pentafluorosulfanyl \(SF₅\) Group Continues to Prove Its Value in Medicinal Chemistry
A new study from Santiago Vázquez, @[Alba López Ruiz](urn:li:person:TrqOGkPNiz) and coworkers at the University of Barcelona highlights an interesting example of how the pentafluorosulfanyl \(SF₅\) group can recover potency during lead optimisation. The study focused on acetanilide-based soluble epoxide hydrolase \(sEH\) inhibitors and demonstrates how strategic substituent selection can dramatically influence biological activity. Using a Topliss-guided optimisation strategy, researchers explored a range of aromatic substituents and found that the pentafluorosulfanyl \(-SF₅\) group consistently enhanced inhibitor potency. The work highlights how SF₅ can outperform more traditional fluorinated groups by offering a unique combination of electronic, steric, and lipophilic properties. For medicinal chemists, this is another strong example of why SF₅-containing building blocks and intermediates are becoming increasingly important in lead optimisation programs. We're excited to support researchers with our range of SF₅-containing building blocks that help accelerate drug discovery and SAR exploration. Our full range of SF₅-containing building blocks can be found using our search tools at https://lnkd.in/eVbfw6Ua Are you incorporating SF₅ chemistry into your medicinal chemistry projects? Full article. Topliss-Guided Optimization of Acetanilide-Based Soluble Epoxide Hydrolase Inhibitors: Exploring the Pentafluorosulfanyl Group as a Potency-Enhancing Motif https://lnkd.in/eiSV\_u7k