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We report herein the design, synthesis, and in vitro anti‐mycobacterial activities of 11 pyrrolidine‐containing or piperazine‐containing nitrofuranylamides. Results revealed that all derivatives 3a–k endowed with excellent activity [minimum inhibitory concentration (MIC): <0.016–0.482 μg/mL] against Mycobacterium tuberculosis (MTB) H37Rv strain and more than half of them were more potent than the first‐line anti‐tuberculosis agents isoniazid (MIC: 0.078 μg/mL) and rifampicin (MIC: 0.078 μg/mL). The most active six derivatives were further evaluated against two clinically isolated multidrug‐resistant MTB strains resistant to both of isoniazid and rifampicin. In particular, four of them 3a, 3c, 3d, and 3j (MIC: 1.412–3.230 μg/mL) showed promising activity against the two clinically isolated multidrug‐resistant MTB strains and could act as starting points for further investigation. [ABSTRACT FROM AUTHOR]

We report herein the design, synthesis, and in vitro anti‐mycobacterial activities of a series of 1,2,3‐triazole‐tetraethylene glycol tethered isatin dimers. Our results indicated that all the synthesized isatin dimers showed weak to moderate anti‐mycobacterial activities against both Mycobacterium tuberculosis H37Rv and multidrug‐resistant tuberculosis strains. Dimer 7g was found to be most active against the tested two strains with minimum inhibitory concentration of 128 and 64 μg/mL, which was eightfold more potent than INH (minimum inhibitory concentration: 512 μg/mL) against multidrug‐resistant tuberculosis. Moreover, dimer 7g (CC50: 62.5 μg/mL) also showed acceptable cytotoxicity against VERO cell line, could act as a lead for further investigation. The enriched structure–activity relationship may pave the way to find more effective anti‐mycobacterial candidates. [ABSTRACT FROM AUTHOR]

A new class of istain dimers tethered by tetraethylene glycol was designed, synthesized, and evaluated for their in vitro anti‐mycobacterial activities against Mycobacterium tuberculosis H37Rv and multidrug‐resistant M. tuberculosis strains. Our results indicated that all the synthesized hybrids exhibited promising anti‐mycobacterial activities against the tested strains and the enriched structure–activity relationship may pave the way to further rational development of istain dimers with a unique mechanism of action different from that of the currently used drugs to overcome the resistance. [ABSTRACT FROM AUTHOR]

Tuberculosis (TB) remains one of the most widespread and leading deadliest diseases, threats one-third of the world's population. Although numerous efforts have been undertaken to develop new anti-TB agents, only a handful of compounds have entered human trials in the past 5 decades. Triazoles including 1,2,3-triazole and 1,2,4-triazole are one of the most important classes of nitrogen containing heterocycles that exhibited various biological activities. Triazole derivatives are regarded as a new class of effective anti-TB candidates owing to their potential anti-TB potency. Thus, molecules containing triazole moiety may show promising in vitro and in vivo anti-TB activities and might be able to prevent the drug resistant to certain extent. This review outlines the advances in the application of triazole-containing hybrids as anti-TB agents, and discusses the structure-activity relationship of these derivatives. [ABSTRACT FROM AUTHOR]