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Cyclic Sulfonamides for Drug Design

Sulfonamides are popular in drug discovery: more than 100 FDA-approved drugs on the market are sulfonamide-containing. Bioactive cyclic sulfonamides (sultams) include the anticonvulsant Sultiame (Bayer) and the anti-inflammatory drug Piroxicam (Pfizer). Mostly, the N-aryl substituted sultams are synthesized from the corresponding anilines. Herein, we present a library of aliphatic sultams that can be easily alkylated at the N-atom. These compounds can be considered as water-soluble mimics of common cyclic amines – pyrrolidines, piperidines, etc.

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