4.6 Article

Design, synthesis and in vitro anti-mycobacterial activities of homonuclear and heteronuclear bis-isatin derivatives

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FITOTERAPIA
卷 127, 期 -, 页码 383-386

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ELSEVIER SCIENCE BV
DOI: 10.1016/j.fitote.2018.03.018

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Isatin; Homonuclear; Heteronuclear; Dimer; Anti-mycobacterial; Structure-activity relationship

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A series of novel homonuclear and heteronuclear bis-isatin derivatives tethered through ethylene were designed, synthesized and evaluated for their in vitro anti-mycobacterial activities against MTB H37Rv and MDR-TB. All hybrids exhibited potential anti-mycobacterial activities against MTB H37Rv and MDR-TB with MIC ranging from 16 to 256 mu g/mL. In particular, the heteronuclear bis-isatin 4i (MIC: 25 and 16 mu g/mL) was most active against MTB H37Rv and MDR-TB strains, and could act as a lead for further optimization.

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