Acylsulfonamides are fundamental scaffolds in pharmaceutical development due to their broad range of biological activities. (1) They are widely recognized as bioisosteres of carboxylic acid groups, attributed to their similar acidity and resistance to chemical and enzymatic hydrolysis. In addition to serving as direct drug motifs, acylsulfonamide scaffolds are extensively utilized in solid-phase peptide synthesis (2) and as acylating agents for amines.
