Tuberculosis (TB) is an infectious disease caused predominantly by bacillus Mycobacterium tuberculosis (MTB). The increasing prevalence of multidrug‐resistant MTB necessitates the discovery and development of alternative drugs against tuberculosis with a new mechanism of action. Over the past years, several benzoxazole derivatives have been synthesized and screened for their biological activity. Interestingly, some of them had promising antitubercular activity. Despite that, none of the benzoxazole derivatives has entered the phase of the preclinical hit‐to‐lead optimization step in anti‐TB research. In this review, we are summarizing recently published articles that evaluate the potency of benzoxazole heterocycle in the development of novel anti‐TB agents and outlined the future aspects of this promising heterocycle.
This
study reports two synthetic approaches leading to 2-aminobenzoxazoles
and their N-substituted analogues. Our first synthetic
strategy involves a reaction between various o-aminophenols
and N-cyano-N-phenyl-p-toluenesulfonamide as a nonhazardous electrophilic cyanating agent
in the presence of Lewis acid. The second synthetic approach uses
the Smiles rearrangement upon activation of benzoxazole-2-thiol with
chloroacetyl chloride. Both developed synthetic protocols are widely
applicable, afford the desired aminobenzoxazoles in good to excellent
yields, and use nontoxic and inexpensive starting material.
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