Abstract Infectious diseases like malaria, tuberculosis or HIV are among the leading causes of death worldwide according to WHO estimations. Nevertheless, the fight against infectious diseases is aggravated through growing development of resistance towards current drugs and due to their severe adverse effects. The introduction of the lipophilic organometallic moiety ferrocene, a compound with a sandwich-like structure, in an existing bioactive molecule is a promising tool for the development of new more efficient drugs with innovative mechanisms of action. Thus, this review summarizes recent developments in the field of ferrocene conjugation to bioactive molecules like natural products, synthetically derived drugs, peptides as well as heterobimetallic complexes. Hereby, we will provide the reader with a summary of the most potent ferrocene derivatives reported for a plethora of infectious diseases by tabulating and critically assessing the corresponding IC50 values and the minimal inhibitory concentrations (MIC). Owing to the diverse field of infectious diseases the reported ferrocene derivatives were classified according to their targets into four main groups: antiparasitic (with antimalarial agents as biggest group), antibacterial, antifungal and antiviral agents.