Benzothiazoles and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antitumor, antimicrobial, antidiabetic, anticonvulsant and anti-inflammatory. These different biological applications for benzothiazole compounds have motivated new efforts in search for novel derivatives with improved biological activity and diverse applications in pharmaceutical industry. Owing to the importance of this system, the aim of this review is to highlight aspects reported on the chemistry and biological activity of benzothiazoles during the past few years (2000-2010).