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Design, synthesis, and biological evaluation of new quinoline-based heterocyclic derivatives as novel antibacterial agents

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Abstract

A novel series of quinolone-based heterocyclic derivatives including thiadiazine, thiadiazoles, and triazole were synthesized and their in vitro antibacterial activity against Gram-positive and Gram-negative bacteria were evaluated. Newly synthesized derivatives have been obtained in good yields ranging from 65 to 80%. The synthesized derivatives have been characterized and their structures identified using spectroscopic analysis including NMR, FT-IR, and mass techniques. Most of compounds exhibited moderate-to-good antibacterial activity against all four bacterial strains and are significantly more active than ampicillin. Compounds showed relatively good anti-bacterial activity compared to moderate activity of other compounds. The results obtained herein are important for further structure modifications of quinoline bearing heterocyclic moiety and the exploitation of the therapeutic potential of quinoline derivatives as antibacterial agents.

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Acknowledgements

Ghazwan Salman would like to express his sincere gratitude to Mustansiriyah University for providing financial support for one sabbatical year. Dhafer S. Zinad would like to express his great thanks to the University of Technology for providing facilities and support. Ahmed Mahal would like to acknowledge financial support through the CAS President’s International Fellowship Initiative (2016PM032), Chinese Academy of Sciences (CAS).

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Authors and Affiliations

  1. Department of Chemistry, College of Sciences, Mustansiriyah University, 10052, Baghdad, Iraq

    Ghazwan Ali Salman

  2. Applied Science Department, University of Technology, Baghdad, 10001, Iraq

    Dhafer S. Zinad

  3. Key Laboratory of Plant Resources Conservation and Sustainable Utilization and Guangdong Provincial Key Laboratory of Applied Botany, South China Botanical Garden, Chinese Academy of Sciences, Guangzhou, 510650, People’s Republic of China

    Ahmed Mahal

  4. Guangzhou HC Pharmaceutical Co., Ltd, Guangzhou, 510663, People’s Republic of China

    Ahmed Mahal

Authors
  1. Ghazwan Ali Salman
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  2. Dhafer S. Zinad
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  3. Ahmed Mahal
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Correspondence to Ghazwan Ali Salman or Ahmed Mahal.

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Salman, G.A., Zinad, D.S. & Mahal, A. Design, synthesis, and biological evaluation of new quinoline-based heterocyclic derivatives as novel antibacterial agents . Monatsh Chem 151, 1621–1628 (2020). https://doi.org/10.1007/s00706-020-02686-3

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  • DOI: https://doi.org/10.1007/s00706-020-02686-3

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