Publication
Title
Design, synthesis and biological evaluation of novel quinoline-based carboxylic hydrazides as anti-tubercular agents
Author
Abstract
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.
Language
English
Source (journal)
Chemical biology and drug design. - Copenhagen, 2006, currens
Publication
Copenhagen : 2016
ISSN
1747-0277 [print]
1747-0285 [online]
1397-002X [opgeheven]
Volume/pages
88:4(2016), p. 585-591
ISI
000383576500012
Full text (Publisher's DOI)
Full text (open access)
The author-created version that incorporates referee comments and is the accepted for publication version Available from 09.09.2017
Full text (publisher's version - intranet only)
UAntwerpen
Faculty/Department
Research group
[E?say:metaLocaldata.cgzprojectinf]
Elucidating the mechanism of action of octahydrobenzo[j] phenanthridinediones as novel potent antimycobacterial compounds.
Publication type
Subject
Affiliation
Publications with a UAntwerp address
External links
Web of Science
Record
Identification
Creation 09.09.2016
Last edited 13.08.2017
To cite this reference