Trifluoromethylated lactams: promising small molecules in the search for effective drugs

Abstract

Lactams are a crucial class of compounds with broad therapeutic applications, including in the treatment of cancer, diabetes, and infectious diseases. Functionalised lactams are essential core structures in numerous alkaloids and pharmaceuticals. The introduction of fluorine-containing groups, such as a trifluoromethyl (CF₃) group, into organic molecules significantly alters their physical and chemical properties. This review highlights the primary biological targets, as well as the most important synthetic pathways, associated with trifluoromethylated β-lactams (four-atom rings), γ-lactams (five-atom rings), δ-lactams (six-atom rings), and ε-lactams (seven atom rings). Furthermore, we analyze the most common lactam scaffolds, evaluating their potential for future chemical synthesis and emphasizing those that merit attention despite having limited reported analogues. This article aims to provide a comprehensive overview of the importance of trifluoromethylated lactams in drug discovery and design.