Abulkhair_2025_Arch.Pharm.(Weinheim)_358_e2500033

Because of its importance in medicinal chemistry, scientific researchers have been interested in incorporating sulfamethazine in developing biologically active candidates. To achieve this, several synthetic approaches have been adopted. The adopted approaches included condensation with electrophilic reactants, coupling with nucleophilic aromatics and active methylene compounds, Knoevenagel condensation, Doebner Miller reaction, microwave-assisted click cycloaddition, green reaction routes, and multicomponent reaction. Linking this molecular scaffold to a variety of heterocycles in the last 10 years furnished a set of potential anti-inflammatory, antiviral, anticancer, antiparkinsonian, neuroprotective, and antidiabetic candidates targeting H5N1 NA, epidermal growth factor receptor, acetylcholinesterase (AChE), butylcholinesterase (BChE), human carbonic anhydrase (hCA), alpha-amylase, and alpha-glucosidase. This review reports all the adopted synthetic approaches, the biological activities studied, structure-activity relationship analyses, and the mechanistic investigations of the reported organic sulfamethazine-incorporating molecules throughout 2015-2024, based on information retrieved from three search engines: Scopus, PubMed, and Google Scholar.