Isoxazole

Isoxazole is a member of the five-membered heterocycle drug scaffold. Isoxazole has been used as a BET bromodomain inhibitor and can improve β-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]}. In Vitro: Isoxazole (20 µM, 48 hours) improves β-cell function by inhibiting excessive proliferation of MIN6 cells (mouse pancreatic β-cells) and altering the gene expression profile of MIN6 cells (enhancing the neuroendocrine phenotype)^[5]. In Vivo: Isoxazole (16 mg/kg, i.p., once daily for 4 weeks) improves β-cell function in diabetes mice model (PANIC-ATTAC mice model induced by dimerizer (e.g., AP20187, HY-13992)^[5].