Synthesis and Antimalarial Bioassay of Quinine – Peptide Conjugates

Authors

  • Siva S. Panda,

    1. Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, FL, USA
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  • Mohamed A. Ibrahim,

    1. Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, FL, USA
    2. Organic Chemistry Department, College of pharmacy, Misr University for Science and Technology, Al-Motamayez District, Egypt
    3. Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt
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  • Hasan Küçükbay,

    1. Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, FL, USA
    2. Department of Chemistry, Faculty of Arts and Sciences, University of Inonu, Malatya, Turkey
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  • Marvin J. Meyers,

    1. Center for World Health and Medicine, Saint Louis University, St. Louis, MO, USA
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  • Francis M. Sverdrup,

    1. Center for World Health and Medicine, Saint Louis University, St. Louis, MO, USA
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  • Said A. El-Feky,

    1. Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt
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  • Alan R. Katritzky

    Corresponding author
    1. Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, FL, USA
    2. Department of Chemistry, King Abdulaziz University, Jeddah, Saudi Arabia
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Abstract

Amino acid and peptide conjugates of quinine were synthesized using microwave irradiation in 52–95% yields using benzotriazole methodology. The majority of these conjugates retain in vitro antimalarial activity with IC50 values below 100 nm, similar to quinine.

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