Nitroimidazoles based compounds remain a hot topic of research in medicinal chemistry due to their numerous biological activities. Moreover, many clinical candidates based on this chemical core have been reported to be valuable in the treatment of human diseases. Metronidazole (MTZ) derived conjugates demonstrated a potential application in medicinal chemistry research over the last decade. In this review, we summarize the synthesis, key structure-activity-relationship (SAR) and associated biological activities such as antimicrobial, anticancer, antidiabetic, anti-inflammatory, anti-HIV and anti-parasitic (Anti-trichomonas, antileishmanial, antiamoebic and anti-giardial) of explored MTZ-conjugates. The molecular docking analysis is also presented simultaneously, which will assist in developing an understanding towards designing of new MTZ-conjugates for target-based drug discovery against multiple disease areas.