Synthesis and Biological Activity of Quinoline-4-Carboxylic Acid

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We have synthesized a series of quinoline hybrid thiosemicarbazide derivatives under microwave irradiation. Synthesized compounds were successfully applied against the biological studies. Compounds 7a 7g 7k exhibited potent activity againstP. aeruginosa compounds 7a 7f7h7r showed excellent activity against E.coli compounds 7a 7b 7c 7e 7f 7l 7o 7p 7q and 7sexhibited good activity against plasmodium falciparum strain. The docking study was performed on selected three proteins 3JSU 4DP3 and 1J3K. Compounds7b (-8.32) and 7i (-8.22) were selected in 3JSU compounds7c (-7.23) and 7l (-5.82) were selected in 4DP3 for the best binding possess compounds7b (-4.323) and 7l (-3.039) were selected in 1J3Kfor the best binding possess. The docking study was suggested that selected molecules were perfect fit into the protein cavity with excellent G-score. Molecular dynamics study of compound 7ewith protein (PDB: 3JSU) studied in Schrodinger software Pharmacophore study and ADME-Tox were carried out for the drug-likeness properties. This study proved that our molecules could be act as hit molecules in the future.
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