Cefprozil complexes with Co(II), Ni(II), Zn(II), Mn(II), Cr(III), Fe(III) and Cu(II) were synthesized. Structure of the synthesized complexes was proved by IR, UV-Vis spectroscopy, magnetic susceptibility, ESR, elemental and thermal analysis methods. The data indicated that cefprozil acts as a bidentate ligand via amide and carboxylate groups in the case of Fe(III) and Cu(II) metal ions and via amide and amino group of side chain in Cr(III), Ni(II), Co(II), Mn(II) and Zn(II) metal ions. From physicochemical and spectroscopic data an octahedral structures were suggested for Co(II), Mn(II), Cr(III), Fe(III) and Cu(II), while Ni(II) and Zn(II) exhibited a tetrahedral geometry. DFT studies confirmed the binding sites of cefprozil as well as energy of HOMO, LUMO and global chemical reactivity descriptors were discussed. The complexes were evaluated for their antimicrobial activity and the results indicated that some complexes have a well considerable activity against the tested microorganisms.