QUINAZOLINE-PURINE DERIVATIVES AS ANTIDIABETICS: SYNTHESIS, IN- SILICO AND IN-VITRO EVALUATION

The study involved condensation of 8-bromo-7-(but 2yn-1yl)-3-methyl-3,7-dihydro-1H-purine-2,6-dione with 2-(chloro methyl)-4-methyl quinazoline. The compound obtained was assigned 3, on which different substitutions were made at 8(th) position, to obtain various derivatives of quinazoline. The obtained derivatives were characterized using I.R, 1H-NMR, 13C-NMR and Mass spectra. For finding antidiabetic activity of all synthesized compounds, they were subjected for their inhibitory activity on a-amylase, using Acarbose as standard and DPP-4 using Metformin as standard. The results obtained, from the activity performed was nearly equal with that of the standards used and synthesized compound 3B was found to possess inhibitory activity. It has also been confirmed by docking studies, that Compound 3B and Metformin when docked on 3 proteins 2ONC, 5Y7J and 2OQV, Compound 3B was found to be most potent drug candidate against DPP-4.