Sulfonamides have been in clinical use for many years, and the development of bioactive
substances containing the sulfonamide subunit has grown steadily in view of their important biological
properties such as antibacterial, antifungal, antiparasitic, antioxidant, and antitumour properties. This
review addresses the medicinal chemistry aspects of sulfonamides; covering their discovery, the structure-
activity relationship and the mechanism of action of the antibacterial sulfonamide class, as well as
the physico-chemical and pharmacological properties associated with this class. It also provides an
overview of the various biological activities inherent to sulfonamides, reporting research that emphasises
the importance of this group in the planning and development of bioactive substances, with a special
focus on potential antitumour properties. The synthesis of sulfonamides is considered to be simple
and provides a diversity of derivatives from a wide variety of amines and sulfonyl chlorides. The sulfonamide
group is a non-classical bioisostere of carboxyl groups, phenolic hydroxyl groups and amide
groups. This review highlights that most of the bioactive substances have the sulfonamide group, or a
related group such as sulfonylurea, in an orientation towards other functional groups. This structural
characteristic was observed in molecules with distinct antibacterial activities, demonstrating a clear
structure-activity relationship of sulfonamides. This short review sought to contextualise the discovery
of classic antibacterial sulfonamides and their physico-chemical and pharmacological properties. The
importance of the sulfonamide subunit in Medicinal Chemistry has been highlighted and emphasised,
in order to promote its inclusion in the planning and synthesis of future drugs.
PHYSICO-CHEMICAL OPTIMIZATION AND STRUCTURE-ACTIVITY RELATIONSHIP STUDIES OF ALDEHYDE-DERIVED N-ACYLHYDRAZONES: TOWARDS THE IMPROVEMENT OF MODERATE METAL CHELATORS AS A STRATEGY AGAINST METAL-ENHANCED AGGREGOPATHIES
