Design, Synthesis and <italic>in vitro</italic> Antimycobacterial Activities of Isatin‐1,2,3‐triazole‐moxifloxacin Hybrids.

A new class of isatin‐1,2,3‐triazole‐moxifloxacin (<bold>MXFX</bold>) hybrids <bold>5a–j</bold> was designed, synthesized, and screened for their <italic>in vitro</italic> antimycobacterial activities against Mycobacterium tuberculosis H37Rv and MDR‐TB. All the synthesized hybrids (MIC: 0.10–0.78 μg/mL) exhibited excellent activities against MTB H37Rv and MDR‐TB, in spite of none of them were more potent than the parent <bold>MXFX</bold> (MIC: 0.10 and 0.12 μg/mL). Against MTB H37Rv, the most active <bold>5f</bold> (MIC: 0.10 μg/mL) was comparable with <bold>MXFX</bold> and 4 times more potent than <bold>RIF</bold> (MIC: 0.39 μg/mL). Against MDR‐TB, all hybrids were more active than <bold>RIF</bold> (MIC: 32 μg/mL) and <bold>INH</bold> (MIC: >128 μg/mL). In particular, hybrid <bold>5e</bold> (MIC: 0.10 μg/mL) was comparable with <bold>MXFX</bold> and 256 and >1,024 times more potent than <bold>RIF</bold> and <bold>INH</bold>. Both conjugates <bold>5e</bold> and <bold>5f</bold> warrant further investigations. [ABSTRACT FROM AUTHOR]