In this study the mononuclear complexes of Cu(II), Zn(II), Zr(IV) and Cd(II) were synthesized by the reaction of antiepileptic pregabalin (Preg) in the presence of 2,2'-bipyridine (Bipy) with molar ratio 1:1:1. The coordination of the two ligands toward metal ions was informed by using elemental analysis, FT-IR, UV-Vis., 1H NMR, XRD, thermal analyses (TG-DTG), molar conductance and magnetic moment. FT-IR and UV-Vis. spectra proved that Preg acts as a bidentate ligand chelated to the metal ions via the oxygen atom of the carboxylic group and nitrogen atom of the amino group and Bipy chelated through the two nitrogen atoms forming octahedral complexes. The thermodynamic parameters (Ea, ΔH*, ΔS* and ΔG*) were calculated by using Coats-Redfern and Horowitze-Metzger method from TG-DTG curves. The antimicrobial activity for all compounds against various species of bacteria and fungi was assayed. Results showed that some metal complexes showed more biological efficiency than the parent ligands.