Substantial attention has been given in developing novel heterocyclic compounds as these have been found to exhibit varied biological activities. Benzothiazoles belong to one of the special categories of heterocyclic compounds with a wide range of biological activities such as antimicrobial, antitumor, antidiabetic, antitubercular, antimalarial, anticonvulsant, anthelmintic, analgesic, antiinflammatory and many more. These compounds have been serving as leads for researchers who are actively involved in synthesizing and evaluating their biological activities. Such an extensive work has stimulated further development of new benzothiazole derivatives with enhanced biological activities. This review focuses on the various approaches on the synthesis of benzothiazole derivatives viz., conventional, green, combinatorial and microwave-assisted methods. It also highlights various biological activities of the currently synthesized benzothiazoles.