Vol2 Paper 12

posted Aug 14, 2018, 2:34 AM by Yaseen Raouf Mohammed   [ updated Sep 4, 2018, 1:41 AM ]

 Narmin Hamaamin Hussen

 College of Pharmacy, University of Sulaimaniya, Iraq

 Ahlam Jamil Qasir

 College of Pharmacy, University of Baghdad, Iraq

Quinolones were conjugated with 7-hydroxycoumarin via the amine group of amino acids by reaction hydrazide group of quinolones –amino acid derivatives with formyl group to carbon 8 of 7-hydroxy-4-methyl coumarin. Synthesis of amino acid methyl esters HCl [N1 and N2], by reaction of amino acid with thionyl chloride in methanol. Synthesis amide derivatives [N3- N6] by reaction amino acid methyl esters HCl [N1 and N2] with quinolones. The DCC/ HOBt coupling reagents used for peptide bond formation. Synthesis of hydrazide derivatives [N7- N10], by reaction [N3- N6] with hydrazine hydratein ethanol. Synthesis of 7-hydroxy -4-methyl coumarin [N11] was achieved by reaction of ethyl acetoacetate with resorcinol .Synthesis of 8-formyl-7-hydroxy-4- methyl coumarin [N12], was achieved by Duff reaction, which is used for synthesis of aromatic aldehyde with hexamine. Synthesis of Hydrazone Derivatives [N13- N16] was achieved by reaction compounds [N7- N10] with compound [N12] in the presence of ethanol.Structure elucidation was confirmed by spectrometric analysis using FT-IR, 13C-NMR and CHN elemental analyzer. Synthesized compounds have been found to exhibit considerable antibacterial activity in vitro. Among the quinolones-coumarin derivatives; compounds [N15&N16] showed the highest rate of inhibition against Staphylococcus aureus than Klebsiella pneumoniae.

Nalidixic acid; Ciprofloxacin; 7-Hydroxycoumarin; Amino acids; Antibacterial activity; DNA gyrase inhibitors.

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