A Patent Review on the Current Developments of Benzoxazoles in Drug Discovery

The benzoxazole moiety is widely found in various natural compounds, which are often found to be biologically active. Due to its versatile biological properties, benzoxazole has been incorporated as an essential pharmacophore and substructure in many medicinal compounds. In the past years, numerous benzoxazole derivatives have been synthesised and evaluated for their biological potential. The wide range in therapeutic potential of benzoxazole derivatives is related to the favourable interactions of the benzoxazole moiety with different protein targets. Herein we review the biological activities of benzoxazole derivatives patented within the past six years. Using the Lens database, granted patents issued from 2015 to 2020 were retrieved. The patented benzoxazole derivatives demonstrated excellent activity against various protein targets and diseases, with some reaching clinical trial stage. Pharmacological and medicinal aspects of patented benzoxazole derivatives are discussed. The recent development and drawbacks are also reviewed.