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Designs, Synthesis, Structural Elucidation And Antimicrobail Evalution Of Various Derivatives Of 2-Mercaptobenzoxazole As Possible Antimicrobial Agents
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SADEQ AL-TAMEEMI , ZUHAIR MUHI-ELDEEN, ELHAM AL-KAISSI, NAJAH AL-MUHTASEB, RAND AL-QAZWEENY, SUMIA SAMER, JAAFAR AL-HUSSEINI
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| Abstract:
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Background: The continuously increasing resistance of pathogenic microorganisms against many of the commonly used antibiotics imposes a considerable effort to develop new drugs. 2-Mercaptobezoxazole (2-MBO) and its derivatives are considered as one of the most important heterocyclic in pharmaceutical chemistry as antimicrobial agent. Methods: This work was aim to synthesized various derivatives of 2-MBO and their structures confirmed through IR, 1H-NMR, 13C-NMR, DSC and elemental analysis. The synthesized compounds were docking with dihydrofolate reductase enzyme (DHFR) showing good binding energy affinity. To evaluate the antimicrobial activity of the synthesized compounds, agar diffusion and broth dilution test were used, against Staphylococcus aureus (ATCC 6538), Bacillus subtilis (ATCC 6633), Escherichia coli (ATCC 8739), Pseudomonas aeruginosa (ATCC 9027), and Candida albicans (ATCC 10231). Results: All synthesized compounds were consistent with DSC, 1H-NMR, 13C-NMR, FT_IR and elemental analysis. Compound 2-[(2-phenylethyl) sulfanyl]-1, 3-benzoxazole ZS6 showed good antimicrobial activity against bacteria with MIC of 7.81 ug/ml, and MBC of 15.62 ug/ml and compound S-1,3-benzoxazol-2-yl O-(isobutyl) carbonothioate ZS1 showed antifungal activity higher than miconazole Conclusions: Our findings indicate the potency of ZS6 and ZS1 as candidate for the development of antimicrobial agent.
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2-Mercaptobenzoxazole, Alkylation, Amidation, Acyl Formation, Antimicrobial
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| DOI:
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https://doi.org/10.31838/ijpr/2021.13.04.012
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