Our aim was to develop novel quinazolino-acetidinone derivatives as potent antioxidant agents which could minimize or inhibit oxidative damage through blocking free radical formation or inhibiting chain reaction. In-silico design of novel analogues were carried out using ACD labs ChemSketch 12.0. Molinspiration software was used to analyse ‘Lipinski Rule of Five’ and drug likeness properties. Five derivatives which obeyed rule of five and having desired physico-chemical properties were synthesized by five step process. After the completion of reaction in each step, the compounds were isolated, recrystallised by using suitable solvents, purified by TLC and column chromatography. Analogues were characterized by FT-IR, H1NMR, C13NMR and Mass Spectroscopy. The Biological evaluation was done by DPPH radical scavenging activity method. The results were compared with effect of standard drug ascorbic acid. The results of present research work showed that novel quinazolino-acetidinone derivatives have comparable antioxidant effect with that of standard antioxidant drug ascorbic acid. This will lead to the development of promising lead compounds for treatment against tumors or other free radical-related diseases