Copper, magnesium and zinc complexes of acetaminophen were synthesized and characterized by infrared spectroscopy, UV- Visible spectroscopy, melting point, X-Ray diffraction analysis and conductivity measurements. On the basis of this study, it is proven that acetaminophen acts as a bidentate ligand coordinated to the metal ions through phenol and carbonyl oxygen atoms. Antibacterial and antifungal activities of the complexes were determined against Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Salmonella typhi, Pseudomonas aeruginosa and Candida albicans. The results indicate that acetaminophen showed activity against Pseudomonas aeruginosa (18 mm and 15 mm) and Staphylococcus aureus (20 mm, 17 mm, 14 mm and 10 mm) respectively. Zinc complex of acetaminophen also showed activity against Pseudomonas aeruginosa (20 mm, 15 mm and 12 mm). Magnesium complex of acetaminophen showed activity against Staphylococcus aureus (19 mm, 15 mm and 13 mm), Salmonella typhi (15 mm and 12 mm) and Pseudomonas aeruginosa (27, 18 and 13 mm). Copper complex of acetaminophen showed activity against Staphylococcus aureus (23 mm, 20 mm, 17 mm and 15 mm), Bacillus subtilis (21 mm, 18 mm, 16 mm and 14 mm), Escherichia coli (22 mm, 19 mm, 17 mm and 14 mm), Salmonella typhi (18 mm, 16 mm, 14 mm and10 mm) and Pseudomonas aeruginosa (24 mm, 21 mm, 19 mm and 16 mm). Acetaminophen, magnesium and zinc complexes of acetaminophen showed the same inhibitory activity (50 mg/mL) against Pseudomonas aeruginosa. Zinc and magnesium complexes showed the same inhibitory strength (50 mg/mL) against Staphylococcus aureus. Copper complex of acetaminophen was found to be the best as it exhibits the lowest minimum inhibitory concentration (12.5 mg/mL). The lethal dose determination (LD50) of zinc, copper and magnesium complexes of acetaminophen were 289 mg/kg, 3808 mg/kg and 1265 mg/kg respectively. The complexes of copper and magnesium were considered slightly toxic while zinc complex of acetaminophen was considered moderately toxic. Anti-inflammatory activity of the synthesized complexes has been carried out by paw edema method in rats. The maximum percentage anti-Inflammatory effects of zinc, magnesium and copper complexes of acetaminophen were 26.9%, 18.9% and 32.4% respectively.