Transition metal complexes of 4-aminoantipyrine derivatives have been gaining great interest due to their rich coordination chemistry and potential applications in the field of pharmaceutical science. The presence of a free amine and a cyclic ketone functionality makes 4-aminoantipyrine an attractive amphoteric substrate for Schiff base formation. Varieties of aldehydes/ketones or amines of versatile steric, electronic and functional nature could be condensed with the 4-aminoantipyrine motif to obtain the ligand systems of multi-denticity and diverse coordination behaviour. The transition metal complexes obtained from these ligand systems exhibit unique structural and functional properties. This review compiles the important transition metal complexes developed from the Schiff base derivatives of 4-aminoantipyrine, and their utility as antibacterial and antifungal agents. Rationale of the strategies involved in the development of highly potential antimicrobial agents is discussed.