Premium
Design, synthesis and biological evaluation of novel quinoline‐based carboxylic hydrazides as anti‐tubercular agents
Author(s) -
Chander Subhash,
Ashok Penta,
Cappoen Davie,
Cos Paul,
Murugesan Sankaranarayanan
Publication year - 2016
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12788
Subject(s) - chemistry , quinoline , cytotoxicity , in silico , in vitro , carboxylic acid , stereochemistry , combinatorial chemistry , selectivity , click chemistry , biochemistry , organic chemistry , gene , catalysis
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 , 1 H NMR , and M ass). The in‐vitro anti‐tubercular activity (against M ycobacterium tuberculosis H 37 R a) 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 μ g/mL. The two most potent compounds of the series, 6j and 6m exhibited MIC values 7.70 and 7.13 μ g/mL, respectively, against M . tuberculosis with selectivity index >26. Structure–activity 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.