Design,synthesis and biological evaluation of novel quinoline‐based carboxylic hydrazides as anti‐tubercular agents |
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| Authors: | Subhash Chander Penta Ashok Davie Cappoen Paul Cos Sankaranarayanan Murugesan |
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| Affiliation: | 1. Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science, Pilani, Rajasthan, India;2. Laboratory of Microbiology, Parasitology and Hygiene (LMPH), S7, Faculty of Pharmaceutical, Biomedical and Veterinary Sciences, University of Antwerp, Wilrijk, Belgium |
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| 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. 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. |
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| Keywords: | cytotoxicity drug likeness fibroblast
Mycobacterium tuberculosis
quinoline |
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