Isoxazole is a member of the five-membered heterocycle drug scaffold. Isoxazole has been used as a BET bromodomain inhibitor and can improve beta-cell function in a diabetic mouse model. Isoxazole and its derivatives exhibit broad biological activities (such as antimicrobial, antibacterial, antifungal, antiviral, anticancer, anti-inflammatory, immunomodulatory, analgesic, anti-tuberculosis, and anti-diabetic effects). For example, the bicyclic Isoxazole can act as an HSP90 inhibitor, and the tricyclic Isoxazole is promising as a selective multidrug resistance protein (MRP1) inhibitor[1][2][3][4][5].