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Title
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Design, synthesis and biological evaluation of novel quinoline-based carboxylic hydrazides as anti-tubercular agents
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Author
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Abstract
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| In this study, seventeen novel quinoline-based carboxylic hydrazides were designed as potential anti-tubercular agents using molecular hybridization approach and evaluated in-silico for drug-likeness behavior. The compounds were synthesized, purified, and characterized using spectral techniques (like FTIR, 1H NMR, and Mass). The in-vitro anti-tubercular activity (against Mycobacterium tuberculosisH37Ra) and cytotoxicity against human lung fibroblast cells were studied. Among the tested hydrazides, four compounds (6h, 6j, 6l, and 6m) exhibited significant anti-tubercular activity with MIC values below 20 μg/mL. The two most potent compounds of the series, 6j and 6m exhibited MIC values 7.70 and 7.13 μg/mL, respectively, against M. tuberculosis with selectivity index >26. Structureactivity relationship studies were performed for the tested compounds in order to explore the effect of substitution pattern on the anti-tubercular activity of the synthesized compounds. |
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Language
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English
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Source (journal)
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Chemical biology and drug design. - Copenhagen, 2006, currens
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Publication
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Copenhagen
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2016
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ISSN
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1747-0277
[print]
1747-0285
[online]
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DOI
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10.1111/CBDD.12788
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Volume/pages
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88
:4
(2016)
, p. 585-591
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ISI
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000383576500012
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Pubmed ID
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27203404
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Full text (Publisher's DOI)
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Full text (open access)
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Full text (publisher's version - intranet only)
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