However, the novel quinazoline derivatives were designed to retain anti-inflammatory and anticonvulsant activities. The derivatives of novel 2-(N-phenyl substituted)-3-alkyl amino-quinazoline-4(3H)-one were synthesized by condensation of Isatoic anhydride with alkyl amine. Total 12 compounds (I5- I16) of the series of derivatives were synthesized by novel drug design approach. Two intermediates were formed during the process. Intermediate I (2-amino-N-(2 aminoethyl) benzamide) and intermediate II {3-(2-aminoethyl)-2- (chloromethyl) quinazoline-4(3H)-one)} were the two intermediates formed during the synthesis of novel molecules. Chemical structure of the novel synthesized compound was confirmed by FT-IR (functional groups), 1HNMR (position of hydrogen), 13CNMR (position of Carbon), LC-MS (mass determination), UV (Purity of compound) and elemental analysis. Molecular docking was done by using Autodocking software, autodock MGL tools and PyMol visualization graphic software. Excellent binding affinity was obtained I7 (-9 kcal/mol) with COX receptor and I13 (-9.3 kcal/mol) with GABA receptor. Excellent Root Mean Square Deviation (RMSD) value was obtained I7 (33.64) with COX receptor and I8 (40.90l) with GABA receptor. These novel synthesized derivatives were evaluated for anti-inflammatory activity with COX receptor. Paw oedema model used for this screening. Compound I8, I10 and I14 shows highest anti-inflammatory activity and I5, I9 and I15 moderate anti-inflammatory activity among all the novel synthesized derivatives due to presence of electron withdrawing groups. Further, these synthesized novel quinazoline derivatives were evaluated for anticonvulsant activities by using of MES method. CompoundI5, I6 and I14showed maximum antiinflammatory activity and compound I8, I10 and I12have moderate anticonvulsant activities.