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• W2766419573 abstract "Ten propylene‐1H‐1,2,3‐triazole‐4‐methylene‐tethered isatin‐moxifloxacin hybrids 5a–j were synthesized via Cu‐promoted azide‐alkyne cycloaddition reaction, and screened for their in vitro anti‐mycobacterial activities against Mycobacterium tuberculosis H 37 Rv and multidrug‐resistant tuberculosis. The results showed that all the synthesized hybrids [minimum inhibitory concentration (MIC): 0.25–4.0 μg/mL] displayed considerable activities against the tested two strains, but all less active than the parent moxifloxacin (MIC: 0.10 and 0.12 μg/mL). The resistance index of the most targets was around 1, suggesting this kind of hybrids could reduce the cross–resistance to some extent. Among them, hybrid 5 g was found most active against Mycobacterium tuberculosis H 37 Rv with MIC of 0.39 μg/mL, which was comparable with rifampicin (MIC: 0.39 μg/mL), while conjugate 5a (MIC: 0.25 μg/mL) was 128– > 512 times more active than rifampicin (MIC: 32 μg/mL) and isoniazid (MIC: >128 μg/mL) against multidrug‐resistant tuberculosis." @default.
• W2766419573 created "2017-11-10" @default.
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• W2766419573 date "2017-10-23" @default.
• W2766419573 modified "2023-09-29" @default.
• W2766419573 title "Design, Synthesis and<i>In Vitro</i>Anti-mycobacterial Activity of Propylene-1H-1,2,3-triazole-4-methylene-tethered Isatin-moxifloxacin Hybrids" @default.
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• W2766419573 doi "https://doi.org/10.1002/jhet.3032" @default.
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