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Synthesis and Anti-Tubercular (Tb) Evaluation of Bis[4-Ethylidineamino[1,2,4]Triazole-3-Thiol] Tethered by 1,4-Dihydropyridine

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Abstract

A new series of 5,5'-(2,6-dimethyl-4-phenyl-1,4-dihydropyridine-3,5-diyl)bis[4-(ethylideneamino)-4H-[1,2,4]-triazole-3-thiol) was synthesized via keto-imine condensation. The structural elucidation of the products was investigated by spectral and elemental techniques. Also, the newly synthesized compounds were evaluated for their in vitro anti-tubercular activity, the sensitive and resistant Mycobacterium tuberculosis. Among sixteen tested compounds, compound (V) is equipotent to the standard drug isoniazid against sensitive Mycobacterium tuberculosis, while compounds (IXb), (VIId), and (IIIf) have promising activity.

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Funding

The authors extend their appreciation to the Deanship of Scientific Research at King Khalid University for funding this work through a General Research Project under grant number (R.G.P.1/205/41).

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Authors and Affiliations

  1. Department of Chemistry, Faculty of Science, King Khalid University, 61413, Abha, Saudi Arabia

    S. Abu-Melha & M. M. Edrees

  2. Department of Organic Chemistry, National Organization for Drug Control and Research (NODCAR), 12311, Giza, Egypt

    M. M. Edrees

  3. Department of Chemistry, Faculty of Science, Cairo University, 12613, Giza, Egypt

    N. A. Kheder, S. M. Riyadh & S. M. Gomha

  4. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, King Khalid University, 61441, Abha, Saudi Arabia

    A. M. Saad

  5. Department of Chemistry, Faculty of Science, Taibah University, 30002, Al-Madinah Al-Munawarah, Saudi Arabia

    S. M. Riyadh

  6. Regional Center for Mycology and Biotechnology, Al-Azhar University, 11754, Cairo, Egypt

    M. M. Abdel-Aziz

  7. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Sinai University, 16020, El Arish, Egypt

    M. A. Abdelmoaz

  8. Department of Chemistry, Faculty of Science, Islamic University of Madinah, 42351, Madinah, Saudi Arabia

    S. M. Gomha

Authors
  1. S. Abu-Melha
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  2. M. M. Edrees
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  4. A. M. Saad
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  5. S. M. Riyadh
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  6. M. M. Abdel-Aziz
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  7. M. A. Abdelmoaz
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  8. S. M. Gomha
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Correspondence to M. M. Edrees or S. M. Gomha.

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This article doesnot contain any studies involving human participants performed by any of the authors and doesnot contain any studies involving animals performed by any of the author.

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The authors declare that they have no conflicts of interest.

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Coresponding autor: e-mail: mastourae@yahoo.com.

Coresponding autor: e-mail: s.m.gomha@gmail.com.

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Abu-Melha, S., Edrees, M.M., Kheder, N.A. et al. Synthesis and Anti-Tubercular (Tb) Evaluation of Bis[4-Ethylidineamino[1,2,4]Triazole-3-Thiol] Tethered by 1,4-Dihydropyridine. Russ J Bioorg Chem 48, 345–352 (2022). https://doi.org/10.1134/S1068162022020029

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