A series of biologically active seven 2r, 4c-diaryl-3-azabicyclo[3.3.1]nonan-9-one-4-aminobenzoyl hydrazone derivatives have been synthesized in good yield. The structures of compounds have been established on the basis of IR, 1 H, 13C NMR, and elemental analysis. The structure–activity relationships (SAR) have been studied by screening of antimicrobial activity over a representative panel of bacterial and fungal strains using two-fold serial dilution method. All these synthesized compounds exhibited significant activities against all bacterial and fungal strains.