Antibacterial Activities of Benzoxazole Derivatives: A Comprehensive Review

ABSTRACT

Globally millions of deaths are happening due to bacterial infections annually. As a consequence, antibiotics are essential to treat bacterial infections. Prolonged and careless use of antibiotics induces antibacterial resistance in bacterial cells. Hence, new antibacterial agents are needed to overcome the problem of resistance. Benzoxazoles are important heterocyclic compounds which show interesting biological activities including antibacterial effects. This review collects articles on antibacterial activities of benzoxazoles reported from 1986 to 2025. These benzoxazoles are active against many Gram‐positive bacteria such as Staphylococcus aureus , Enterococcus faecalis , Bacillus subtilis , Methicillin‐resistant S. aureus (MRSA), Mycobacterium tuberculosis , Mycobacterium kansasii , Mycobacterium avium , Bacillus cereus , Streptococcus pneumoniae , Bacillus megaterium , Micrococcus luteus , Streptococcus pyogenes , Enterococcus faecium , and Staphylococcus epidermidis . Besides, they are also active against Gram‐negative bacteria like Escherichia coli , Klebsiella pneumoniae , Acinetobacter baumannii , Serratia marcescens , Vibrio parahaemolyticus , Proteus mirabilis , Salmonella enterica , Proteus vulgaris , Pseudomonas syringae , Pseudomonas aeruginosa , and Vibrio cholerae . Benzoxazoles tethered with other heterocycles like pyrazoles, piperazine, morpholine, piperidine, oxadiazole and triazole exhibited promising antibacterial activity. Further, effects of presence of functional groups such as azo, thioether, thiol, hydrazine, hydrazone, imine and sulfonyl are also discussed. We shed light on pharmacophores responsible for antibacterial effects on the above mentioned bacteria in this review.