A comprehensive review in current developments of benzothiazole-based molecules in medicinal chemistry

•A brief outline on the structure of benzothiazole and its isomers.•This article focuses on the pharmacological profile of benzothiazole.•The structure activity relationships of the benzothiazole derivatives were discussed.•This review will be further helpful for medicinal chemists in designing future drugs.

Benzothiazole (BTA) and its derivatives are the most important heterocyclic compounds, which are common and integral feature of a variety of natural products and pharmaceutical agents. BTA shows a variety of pharmacological properties, and its analogs offer a high degree of structural diversity that has proven useful for the search of new therapeutic agents. The broad spectrum of pharmacological activity in individual BTA derivative indicates that, this series of compounds is of an undoubted interest. The related research and developments in BTA-based medicinal chemistry have become a rapidly developing and increasingly active topic. Particularly, numerous BTA-based compounds as clinical drugs have been extensively used in practice to treat various types of diseases with high therapeutic potency. This work systematically gives a comprehensive review in current developments of BTA-based compounds in the whole range of medicinal chemistry as anticancer, antibacterial, antifungal, antiinflammatory, analgesic, anti-HIV, antioxidant, anticonvulsant, antitubercular, antidiabetic, antileishmanial, antihistaminic, antimalarial and other medicinal agents. It is believed that, this review article is helpful for new thoughts in the quest for rational designs of more active and less toxic BTA-based drugs, as well as more effective diagnostic agents and pathologic probes.

Graphical abstractThe present work systematically gives a comprehensive review in current developments of benzothiazole-based compounds in the whole range of medicinal chemistry and the perspectives that they hold for future research.Figure optionsDownload full-size imageDownload as PowerPoint slide