Guangqiang Bai, Xing Huang, Yong He
Coumarins and pyrazoles are two essential heterocyclic scaffolds in medicinal chemistry, which are extensively applied in the drug discovery and development process owing to their various biological activities. Through the molecular heterocyclic strategy to construct coumarin-pyrazole hybrid heterocyclic molecules, the pharmacokinetic and pharmacodynamic characteristics of the parent compounds can be effectively optimized. According to the structural connection modes, these heterocyclic compounds can be categorized into three main types: fused type, condensed type, and heterocyclic type linked by connecting groups. Among these categories, the condensed type and the linked type can be further subdivided according to the connection positions on the coumarin skeleton, such as derivatives substituted at the C3, C4, C6, C7, and C8 positions. This review summarizes the biological activities, structure-activity relationships (SAR), and action mechanisms of different types of coumarin-pyrazole heterocyclic compounds, intending to provide a reference for the design of novel drugs based on this heterocyclic framework.