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Design, Synthesis and in vitro Antimycobacterial Activities of Isatin‐1,2,3‐triazole‐moxifloxacin Hybrids
Author(s) -
Hu YuanQiang,
Xu Zhi,
Qiang Min,
Lv ZaoSheng
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.3023
Subject(s) - antimycobacterial , moxifloxacin , isatin , chemistry , in vitro , minimum inhibitory concentration , mycobacterium tuberculosis , triazole , microbiology and biotechnology , tuberculosis , antibiotics , biology , medicine , biochemistry , organic chemistry , pathology
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.