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Synthesis and evaluation of some novel tetrahydropyrimidine derivatives as antimicrobial and cytotoxic agents

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Abstract

Starting from the reaction of ethyl cyanoacetate with thiourea and the appropriate aldehydes, a series of new thiopyrimidine derivatives were prepared. Antibacterial evaluation results revealed that compounds 12b, 4c and 11b gave the highest antibacterial activity against all tested bacterial strains. Also, some of the novel compounds were evaluated as cytotoxic agents against liver cancer (HEPG2) cell line. It was noticed that some of the derivatives induced significant growth inhibition with IC50 values (ranged from 6.35 to 9.38 μg/mL) in comparison to 5-Fluorouracil after treatment (IC50: 5 μg/mL).

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Authors and Affiliations

  1. Therapeutical Chemistry Department, National Research Center, Dokki, Cairo, Egypt

    Mogedda E. Haiba, Omar A. Fathalla, Abdel-mohsen M. Soliman & Walaa S. El-serwy

  2. Pharmacetical Chemistry Department, College of Pharmacy, King Saudi University, Riyadh, 11451, Saudi Arabia

    Mogedda E. Haiba

  3. Organic Chemistry Department, Faculty of Science, Minufiya University, Shebin El-Kom, Egypt

    Ibrahim F. Zeid

  4. Microbiology and Immunology Department, National Research Center, Dokki, Cairo, Egypt

    Sherein I. Abd El-Moez

Authors
  1. Mogedda E. Haiba
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  2. Omar A. Fathalla
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  3. Ibrahim F. Zeid
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  4. Abdel-mohsen M. Soliman
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  5. Sherein I. Abd El-Moez
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  6. Walaa S. El-serwy
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Correspondence to Omar A. Fathalla.

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Haiba, M.E., Fathalla, O.A., Zeid, I.F. et al. Synthesis and evaluation of some novel tetrahydropyrimidine derivatives as antimicrobial and cytotoxic agents. Res Chem Intermed 39, 3763–3774 (2013). https://doi.org/10.1007/s11164-012-0879-0

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  • DOI: https://doi.org/10.1007/s11164-012-0879-0

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