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Synthesis, anti-microbial evaluation, and molecular modeling of new pyrazolo[3,4-d]pyrimidine derivatives

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Abstract

Synthesis of some new pyrazolo[3,4-d]pyrimidine derivatives using readily available starting materials are described. A one-pot multi component cyclocondensation reaction was used to prepare the novel 3-methyl-4-aryl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidine-6-thiol which served as a new starting material for all new compounds in this research. The anti-microbial activities of the selective synthesized compounds have been evaluated. Some of the newly prepared compounds were found to have moderate to strong anti-microbial activity, e.g., compound 4a, 6a, and 8, in comparison to the reference drugs. Molecular modeling of the most three biologically active new compounds 4a, 6a, and 8 compared to the reference drugs tobramycin and fluconazole was carried out using Fieldalign 2.0 software.

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Authors and Affiliations

  1. Medicinal Chemistry Department, National Research Centre, Dokki, Cairo, Egypt

    Ahmad F. Eweas & O. A. Fathalla

  2. Pharmaceutical Chemistry Department, College of Pharmacy, Taif University, Taif, Kingdom of Saudi Arabia

    Ahmad F. Eweas

  3. Photochemistry Department, National Research Centre, Dokki, Cairo, Egypt

    S. A. Swelam

  4. Department of Natural and Microbial Products, National Research Centre, Dokki, Cairo, Egypt

    N. M. Fawzy

  5. Department of Microbiology and Immunology, National Research Centre, Dokki, Cairo, Egypt

    Sh. I. Abdel-Moez

Authors
  1. Ahmad F. Eweas
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  2. S. A. Swelam
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  3. O. A. Fathalla
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  4. N. M. Fawzy
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  5. Sh. I. Abdel-Moez
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Correspondence to Ahmad F. Eweas.

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Eweas, A.F., Swelam, S.A., Fathalla, O.A. et al. Synthesis, anti-microbial evaluation, and molecular modeling of new pyrazolo[3,4-d]pyrimidine derivatives. Med Chem Res 21, 3848–3857 (2012). https://doi.org/10.1007/s00044-011-9911-y

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  • DOI: https://doi.org/10.1007/s00044-011-9911-y

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