Acylsulfonamide is a functional group in organic chemistry that is sometimes used in medicinal chemistry. [1] It consists of a sulfonamide group (SO2NH) linked to an acyl group (RCO), forming the structure R−CO−NH−SO2−R′. 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. Examples include: