This paper investigates the synthesis of quinoline derivatives, as well as their molecular routes and broad-spectrum antibacterial uses, with a particular emphasis on the potential of these compounds in contemporary medication development. Since the beginning of time, quinoline derivatives, which are well-known for their structural plasticity, have been an essential component in the treatment of illnesses brought on by bacteria, fungus, and protozoa. The study focusses on a number of different synthetic methodologies, some of which are more conventional, such as the Skraup and Friedländer synthesises, while others are more recent, such as microwave-assisted synthesis and biocatalysis. The mechanistic insights of quinoline derivatives are also investigated in this work. In particular, the capacity of these compounds to block crucial enzymes such as DNA gyrase and topoisomerase, which are necessary for the replication of microorganisms, is investigated specifically.