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Tetraethylene Glycol Tethered Heteronuclear Bis‐isatin Derivatives: Design, Synthesis, and In Vitro Anti‐mycobacterial Activities
Author(s) -
Zhao ShuangQi,
Xu Yan,
Guan Jianguo,
Zhao Shijia,
Zhang GuangDe,
Xu Zhi
Publication year - 2018
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.3255
Subject(s) - heteronuclear molecule , isatin , chemistry , cytotoxicity , mycobacterium tuberculosis , rifampicin , vero cell , in vitro , isoniazid , stereochemistry , tuberculosis , antibiotics , organic chemistry , nuclear magnetic resonance spectroscopy , biochemistry , medicine , pathology
A series of novel tetraethylene glycol tethered heteronuclear bis‐isatin derivatives 7a – l were designed, synthesized, and evaluated for their in vitro anti‐mycobacterial activities against Mycobacterium tuberculosis (MTB) H37Rv and multidrug‐resistant TB (MDR‐TB) as well as cytotoxicity in VERO cell line. All hybrids exhibited potential anti‐mycobacterial activities against MTB H37Rv and MDR‐TB, and acceptable cytotoxicity. Among them, the heteronuclear bis‐isatin 7l [minimum inhibitory concentration (MIC): 16 and 16 μg/mL] was found to be most active against MTB H37Rv and MDR‐TB strains, which was 2‐fold and >8‐fold, respectively, more potent than were the first‐line anti‐tubercular agents rifampicin (MIC: 32 μg/mL) and isoniazid (MIC: >128 μg/mL) against MDR‐TB, also demonstrated acceptable cytotoxicity profile (CC 50 : 62.5 μg/mL), could act as a starting point for further optimization.