Abstract: Piperidinylthiazole derivatives were originally used in the drug discovery. After the commercialization of oxathiapiprolin which was developed as the first piperidinyl thiazole isoxazoline fungicide by DuPont in 2008, piperidinylthiazole compounds were found to inhibit fungi growth by affecting the metabolism of cholesterol through inhibiting its novel target of oxysterol binding protein (OSBP). OSBP-based piperidinylthiazole derivatives were gradually becoming one of the hot research areas for novel pesticide discovery. The development of piperidinylthiazole compounds in the fields of pesticide and medicine, and the research progress of OSBP and oxathiapiprolin in the past decade were summarized in this review to provide reference for the further development of novel pesticides.