Synthesis and determination of pharmacological properties of some novel 8-piperazinylxanthine derivatives

Xanthine (1H-purine-2,6(3H,7H)-dione) derivative compounds can be obtained in nature as compounds such as caffeine, theophylline, theobromine or as synthetic derivatives. These compounds have various pharmacological activities such as anticancer, antiasthma, antiparkinson, anti-Alzheimer, analgesic, diuretic, antitussive, antimicrobial, antidiabetic effects. Linagliptin, a xanthine derivative compound with antidiabetic effects, has a higher inhibitory activity on the dipeptidyl peptidase 4 (DPP-4) enzyme than all other DPP-4 inhibitory compounds. Based on this high efficiency of the linagliptin compound, 15 new xanthine derivative compounds were synthesized. As a result of the examination of the data obtained by the physical analysis and spectral studies on these compounds, the structure illumination process was performed and the purity was examined. The molecular docking process was performed on the synthesized compounds over the active site of the DPP-4 enzyme and the obtained poses and scores were evaluated. The in vitro DPP-4 inhibitory activities of the compounds were evaluated by means of the DPP-4 enzyme kit, and the data obtained showed that 6b and 6c compounds had the highest inhibitory activity against this enzyme.