Benzoxaboroles: New emerging and versatile scaffold with a plethora of pharmacological activities

Benzoxaboroles are versatile boron heterocyclic compounds that have demonstrated a plethora of pharmacological activities including anti-fungal, anti-inflammatory, anti-malarial, anti-trypanosomal, ectoparasiticide, anti-cancer, anti-pneumococcal as well as anti-tubercular. The potential therapeutic profile of benzoxaboroles has led to the fast development of benzoxaborole chemistry and the development of novel strategies for the synthesis of a variety of benzoxaboroles. Some of the benzoxaborole based lead candidates with excellent pharmacological activities have been tested clinically for the treatment of numerous diseases. FDA has recently approved drugs that possess benzoxaborole moieties such as Tavaborole for toenail onychomycosis and Crisaborole for atopic dermatitis. These advancements have carved a new way for benzoxaborole as an attractive and remarkable scaffold in medicinal chemistry worldwide. This review focuses on the major developments in benzoxaborole chemistry, synthetic approaches, physical properties as well as pharmacological importance including structure-activity relationship and mechanism of action of this class of compounds. (C) 2021 Published by Elsevier B.V.