Synthesis and biological evaluation of novel azetidine derivatives as dopamine antagonist

In this study, azetidine derivatives were evaluated for their potency as dopaminergic antagonist. The study comprised derivatives substituted in 3-position with amide moiety. Further, the phenyl moiety of amide was modified at 2, 3, or 4-position. The substituted compounds were biologically evaluated for their affinity for D 2 and D 4 receptors. The most potent D 2 and D 4 antagonist among these compounds appeared to be the N -(1-benzhydryl-azetidin-3yl)-2-bromo-benzamide and N -(1-benzhydryl-azetidin-3yl)-4-bromo-benzamide, respectively. Various docking interactions of CPPMA with the D 4 receptor and the same for compound 5 i.e., N -(1-benzhydryl-azetidin-3yl)-4-bromo-benzamide were found to have good correlation with observed biological activity.