Accelerated research in the field of Co-ordination chemistry has vitalize the scientists world over to consider transition metals as possible powerful agents to enhance the pharmacological activities of different drugs. Additionally, it has been explored that accompaniment of transition metal ions to a drug not only potentiates the already known pharmacological action of the drug but may also be responsible for exhibition of newer activities of the compound unnoticed hitherto. Medicinal inorganic chemistry is flourishing with successful clinical application of many metal complexes. Based on these findings the present work aims at synthesizing various transition metal complexes of some reputable and well practiced pharmacological agents. The drugs included antimicrobial agents, Isoniazid and Pyraziamide, antihypertensive agent, Losartan, antimycotic Fluconazole and oral hypoglycemic agent, Biguanide Metformin. Copper, Nickle, Cobalt, Mangnese, Iron and Cadmium ions were used for complex formation. The structures and characterization of all synthesized complexes were established and characterized by using FTIR, UV-visble, NMR, elemental analysis, AA, SEM and XRD data and their physicochemical properties was done by melting point, color, solubility, conductance and magnetic susceptibility values. The metal complexes of Isoniazid and Pyrazinamide were evaluated for their antimycobacterial activity against Mycobacterium strains resistant to commonly used anti tuberculous agents. Furthermore, all complexes were evaluated for their cytotoxic, antiplatelet and antibacterial activities. Cobalt complex of Pyrazinamide were found active against all resistant tuberculous mycobacterium strains while the Mangnese complex of this drug showed anti mycobacterial activity against two of the strains. All complexes of Isoniazid demonstrated activity against resistant strains of Mycobacterium Tuberculosis, Copper complex of Fluconazole exhibited cytotoxic activity against all four cancer cell lines whereas Cobalt and Iron complexes were cytotoxic against KB-3-1 cancer cell line. Pure Losartan was also found to be cytotoxic against cervical carcinoma cell lines. Contrary to these findings, Biguanide metformin metal complexes were inactive in terms of cytotoxic, antibacterial and antipletelet activities depicting no encouraging results.