Aminoguanidine (Agun) in aqueous solution neutralizes H4edta (ethylenediaminetetraacetic acid) and H4cdta (cyclohexanediaminetetraacetic acid) and replaces two acidic protons with lower pKa values to yield new salts such as diaminoguanidinium dihydrogenethylenediaminetetraacetate trihydrate, (Agun)2H2edta.3H2O (L1) and diaminoguanidiniumdihydrogencyclohexanediaminetetraacetate, (Agun)2H2cdta.H2O (L2) respectively. Two new copper(II) complexes, (Agun)[Cu(Hedta)].3H2O (C1) and (Agun)[Cu(Hcdta)].H2O (C2) have been prepared using the above ligands by the aqueous reaction between the respective ligand and copper(II) nitrate tetrahydrate in 2:1 ratio. The composition of the salts and complexes wasdone by using the basis of hydrazine, analytical and spectral techniques such as elemental analyses, IR, UV-Visible, TG-DTA, in which conformed their formation. Single crystals of (L1), (C1) and (C2) were isolated and their structures were determined by X-ray crystallography. The structure of compound L1 reveals that this salt exists as a zwitterion in solid-state. The structural data of C1and C2shows some interesting features. Aminoguanidinium cation acts as a charge neutralizing species which is quite expected due to the steric reasons and hence could not be accommodated in the primary coordination sphere. Water molecules and aminoguanidine ion are involved in hydrogen bonding interactions and present in the secondary coordination sphere. The compound strongly bound to CT-DNA (Calf-Thymus DNA) through intercalation. The complexes have shown significant growth inhibitory activity against selected types of bacteria namely S. pneumoniae, S. aureus, A. baumannii, P. aeruginosa, K. pneumonia, and five fungi namely C. albicans, C. tropicalis, T. rubrum, A. niger, A. fumigatus. Tests on cell proliferation of human breast cancer cell lines (MCF-7), human lung cancer lines (A-549) and human cervical cell lines (HeLa) were performed for all the compounds. The new water-soluble complexes overcome cisplatin resistance in the MCF-7, A-549, and HeLa cell lines. All the compounds were found to be non-toxic against human normal keratinocyte cells (HaCaT). The biological studies indicated that the complex C4 exhibited better activity among the compounds and the complexes exhibited biological activity in the following order C2>C1>L2>L1.