Acylsulfonamide

[1] It consists of a sulfonamide group (SO2NH) linked to an acyl group (RCO), forming the structure R1-CO-NH-SO2-R2.

This moiety is found in several biologically active molecules and marketed drugs, serving as an useful pharmacophore.

[2] Acylsulfonamides are of particular interest due to their ability to act as bioisosteres of carboxylic acids, offering similar hydrogen bonding capabilities and comparable pKa values (typically between 3.5-4.5).

[2] They are incorporated in various drugs candidates targeting conditions such as bacterial infections, pain, and cancer.

[3] The following are approved drugs that contain the acylsulfonamide functional group: Several investigational new drugs contain also the acylsulfonamide functional group.