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Eight novel 1H‐1,2,3‐triazole‐tethered ciprofloxacin (CPFX) isatin conjugates 5a–h with greater lipophilicity compared with CPFX were designed, synthesized, and evaluated for their in vitro anti‐mycobacterial activity against Mycobacterium smegmatis and Mycobacterium tuberculosis (MTB) H37Rv. The preliminary results showed that all hybrids (MIC: 12.5–100 μg/mL) exhibited considerable activity against M. smegmatis, but less active than the parent CPFX (MIC: 6.25 μg/mL) and the reference INH (MIC: 0.78 μg/mL). Against MTB H37Rv, all hybrids displayed excellent inhibitory activity with MICs ranging from 1.56 to 25 μg/mL, particularly, 5h (MIC: 1.56 μg/mL) was twofold more active CPFX (MIC: 3.12 μg/mL), warrant further investigations.

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A new class of isatin-1,2,3-triazole-moxifloxacin (MXFX) hybrids 5a-j was designed, synthesized, and screened for their in vitro antimycobacterial activities against Mycobacterium tuberculosis H 37 Rv and MDR-TB. All the synthesized hybrids (MIC: 0.10-0.78 μg/mL) exhibited excellent activities against MTB H 37 Rv and MDR-TB, in spite of none of them were more potent than the parent MXFX (MIC: 0.10 and 0.12 μg/mL). Against MTB H 37 Rv, the most active 5f (MIC: 0.10 μg/mL) was comparable with MXFX and 4 times more potent than RIF (MIC: 0.39 μg/mL). Against MDR-TB, all hybrids were more active than RIF (MIC: 32 μg/mL) and INH (MIC: >128 μg/mL). In particular, hybrid 5e (MIC: 0.10 μg/ mL) was comparable with MXFX and 256 and >1,024 times more potent than RIF and INH. Both conjugates 5e and 5f warrant further investigations.

A set of propylene-tethered isatin dimmers 2a-i was synthesized via click chemistry and screened for their in vitro antimycobacterial activities against Mycobacterium tuberculosis (MTB) H 37 Rv and multidrugresistant TB. In spite of all dimmers (minimum inhibitory concentration: 25-> 128 μg/mL) only exhibited weak to moderate activities against the tested MTB H 37 Rv and multidrug-resistant TB, the structure-activity relationship was enriched and the results warrant further development of the anti-TB properties of this kind of dimmers.

in Wiley Online Library (wileyonlinelibrary.com).Isatin and coumarin derivatives with potential anti-tubercular activity, while (thio)semicarbazide/oxime and 1H-1,2,3-triazole moieties exhibited favorable properties such as hydrogen bonding and/or metal chelation capability, so integration of the four pharmacophores into one molecule may provide more effective anti-tubercular candidates. Based on the consideration earlier, 12 isatin-(thio)semicarbazide/ oxime-1H-1,2,3-triazole-coumarin hybrids 8a-l were designed, synthesized, and evaluated for their in vitro anti-mycobacterial activities against M. tuberculosis (MTB) H 37 Rv and MDR-TB. The results showed that all the hybrids (MIC: 50->200 μg/mL) exhibited weak to moderate inhibitory activity against MTB H 37 Rv and MDR-TB, which were far less potent than the references isoniazid (MIC: 0.05 μg/mL) and rifampicin (MIC: 0.39 μg/mL) against MTB H 37 Rv. The most active hybrid 8h (MIC: 50 μg/mL) was comparable with rifampicin (MIC: 32 μg/mL) and more active than isoniazid (MIC: >128 μg/mL) against MDR-TB, could be act as a lead for further optimization. Moreover, the enriched structure-activity relationship paved the way to the further rational development of this kind of hybrids.