Yadav, V., Kumar, R., Srikrishna, S., Prasad, V. (2025). Desulfonylative halogenation of arene sulfonyl chlorides using N-halosuccinimides: Synthesis, molecular docking, and anti-Alzheimer activity.  Bioorg. Med. Chem. Lett. 128(): 130321.

FBrf0263287

Research paper

Considering the significant biological potential of halogenated arenes, we developed a novel and eco-friendly method for accessing dihalogenated arenes viaN-halosuccinimide-promoted desulfonylative halogenation of arenesulfonyl chlorides under metal-free conditions. In silico evaluations of selected compounds for amyloid-beta (Aβ) protein interactions identified compounds 1d and 2d as promising candidates, exhibiting strong binding potential and low toxicity in wild-type Oregon R flies. Furthermore, these compounds demonstrated significant neuroprotective activity in an Aβ-induced Alzheimer's disease model in Drosophila, emphasizing the need for further studies in higher organisms and detailed mechanistic investigations.