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A series of novel 3‐amidophenols with 5‐heteroatomic substitutions were designed and synthesized. Several compounds showed potent antitubercular activity against Mycobacterium tuberculosis H37Ra (MIC = 0.25–5 μg/mL). Compounds 12j and 14i also displayed good… Click to show full abstract
A series of novel 3‐amidophenols with 5‐heteroatomic substitutions were designed and synthesized. Several compounds showed potent antitubercular activity against Mycobacterium tuberculosis H37Ra (MIC = 0.25–5 μg/mL). Compounds 12j and 14i also displayed good inhibitory activity against M. tuberculosis H37Rv and two clinically isolated multidrug‐resistant M. tuberculosis strains (MIC = 0.39–3.12 μg/mL). The privileged compound 14i showed certain oral efficacy on a mouse infection model. The compounds are non‐cytotoxic against L‐O2 hepatocytes and RAW264.7 macrophagocytes. They did not exert inhibitory activity against representative Gram‐positive and Gram‐negative bacteria.
Journal Title: Archiv der Pharmazie
Year Published: 2019
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