Biological activity Study for some heterocyclic compounds and their impact on the gram positive and negative bacteria

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Abstract

In this study eleven novel heterocyclic compounds were prepared and determined their structure by measuring melting point and infrared spectrum for each one. The fourth, fifth and seventh derivatives heterogeneous rings were prepared from reactance of benzotriazole which represent the compounds (6,7,8,9,11) described in scheme (1) with chloro ethyl acetate ester results from the interaction of (1) then reactance ester with aqueous hydrazine for hydrazine (2). Through reactance of hydrazine with benzaldehyde the hydrazone (compound 5) was produced. Azatidine-2-one was obtained from interaction of hydrazine with triethyl amine (TEA). Thiazoldine-4-one was produced from reactance of hydrazone with thioglycolic acid. The derivative 1,3,4-oxadiazole was prepared through reactance of hydrazide with benzoic acid in present of phosphorous oxachloride. Also oxazine-4,7-dione was obtained from reactance of hydrazone with malic anhydride. Finally 1,3,4-Thiadiazole was resulted from reactance ofthiosemicarbazide (perpetrated from reaction isothiocyanate with hydrazide in present of ethanol as solvent) with concentrated Sulfuric acid. The synthesized compounds have been screened for antibacterial activity against nine bacterial isolates (six of them were gram negative: Escherichia coli; Klebsiella pneumoniae; Shigella flexeneri; Proteus mirabilis; Pseudomonas aeruginosa; Acinetobacter baumani, three of them gram positive cocci: Staphylococcus aureus; Streptococcus agalactiae; Enterococcus feacalis). and one isolates of yeast which was Candida albicans. The results appeared that the compound 5 w as t he m ost effective against tested gram positive and negative bacteria following by the compound 3 which had less activity. The other nine compounds had no inhibitory effect against tested bacteria. Finallyno one of the 11 compounds had any activity against C. albicans. Conclusion: Compound 5 is broad spectrum and most efficient antibacterial compared to the others synthesized compounds and control antibiotics, Recommendation: Studying in vivo toxicity of compound No. 5.

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Saleh, S. S., AL-Salihi, S. S., & Mohammed, I. A. (2019). Biological activity Study for some heterocyclic compounds and their impact on the gram positive and negative bacteria. In Energy Procedia (Vol. 157, pp. 296–306). Elsevier Ltd. https://doi.org/10.1016/j.egypro.2018.11.194

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