Jinchao Shi, Xiang Zhu, Junkai Li
Phenylthiazole (PT) is a privileged scaffold with broad potential in medicinal and agrochemical discovery. This review summarizes advances in PT-based bioactive compounds reported from 2013 to 2025, with emphasis on structural modification, biological targets, mechanisms of action, and structure-activity relationships. Comparative analysis shows that the biological performance of PT derivatives is strongly influenced by substitution patterns on the phenyl and thiazole rings, heterocycle incorporation, and linker optimization. PT-based compounds have demonstrated diverse pharmacological and pesticidal activities, confirming the versatility of this scaffold for rational molecular design. However, medicinal applications are substantially more developed than agrochemical uses, particularly in herbicide discovery and other underexplored areas. Overall, PT represents a valuable platform for developing potent, selective, and multifunctional bioactive molecules and offers considerable opportunities for future pesticide innovation.