Schizophrenia is a psychiatric illness characterized by a change in mental acceptance of thoughts. Atypical antipsychotics affect serotonin and dopamine levels by acting on the 5HT2A and D2 receptors, respectively. The aim of this study was to create a new sequence of 3[(2-aminopyridin-1(4H)-yl) diazenyl] quinazolin-4(3H)-one derivatives by designing and synthesizing them. Atypical antipsychotics' biological potential was determined by testing the synthesized derivatives for antagonistic action against dopamine D2 and serotonin 5HT2A. Molecules 5b, 5c, 5e, 5f, and 5j were discovered to be significantly active.