Synthesis,antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety |
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Authors: | Sumesh Eswaran Prasad Shivarudraiah Shridhar Narayanan Sangeetha Subramanian |
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Affiliation: | 1. Anthem Biosciences Pvt. Ltd, 49 Bommasandra Industrial Area, Bommasandra, Bengaluru 560099, Karnataka, India;2. Foundation for Neglected Disease Research, Bengaluru 562157, Karnataka, India;3. SBST, Vellore Institute of Technology, Vellore 632014, Tamil Nadu, India |
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Abstract: | Tuberculosis is the infectious disease caused by mycobacterium tuberculosis (Mtb), responsible for the utmost number of deaths annually across the world. Herein, twenty-one new substituted 1,2,4-oxadiazol-3-ylmethyl-piperazin-1-yl-quinoline derivatives were designed and synthesized through multistep synthesis followed by in vitro evaluation of their antitubercular potential against Mtb WT H37Rv. The compound QD-18 was found to be promising with MIC value of 0.5?µg/ml and QD-19 to QD-21 were also remarkable with MIC value of 0.25?µg/ml. Additionally, we have carried out experiments to confirm the metabolic stability, cytotoxicity and pharmacokinetics of these compounds along with kill kinetics of QD-18. These compounds were found to be orally bioavailable and highly effective. Altogether, these results indicate that QD-18, QD-19, QD-20 and QD-21 are promising lead compounds for the development of a novel chemical class of antitubercular drugs. |
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Keywords: | Quinoline Oxadiazole Antitubercular activity Cytotoxicity Bioavailability |
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