International Journal of Pharmacy and Chemistry

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Screening Investigation of Novel 1,2,4-Triazole-3-Thione Derivatives on Anticonvulsant Activity

Received: 30 August 2016    Accepted: 19 October 2016    Published: 10 January 2017
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Abstract

1,2,4-triazole and its derivatives are present in many biologically active aromatic compounds that have different biological properties and clinical applications including anticonvulsant activity. The number of studies in this direction is increasing. Therefore, based on the results of previous computer predictions, 8 novel 1,2,4-triazole-3-thione derivatives have been synthesized in the Department of Pharmaceutical Chemistry at the National Pharmacy University of Ukraine. The screening test of novel 1,2,4-triazole-3-thione derivatives on anticonvulsant activity in PTZ-induced seizures was conducted on mice. Among test substances revealed were those, which in the dose of 100 mg/kg showed moderate anticonvulsive effect and which were non-inferior to "reference drug" sodium valproate by some parameters. Screening results have confirmed the reasonability of in-depth anticonvulsive activity study of substances-leaders, pharmacological study of their mechanism of action, spectrum of anticonvulsant activity, concurrent types of pharmacological activity, dose-dependence of effect and safety.

DOI 10.11648/j.ijpc.20160202.18
Published in International Journal of Pharmacy and Chemistry (Volume 2, Issue 2, November 2016)
Page(s) 47-51
Creative Commons

This is an Open Access article, distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution and reproduction in any medium or format, provided the original work is properly cited.

Copyright

Copyright © The Author(s), 2024. Published by Science Publishing Group

Keywords

Pharmacological Screening, Anticonvulsant Activity, Triazole Derivatives, PASS-Software, Pentylenetetrazole-Induced Seizures

References
[1] England M. J. Epilepsy Across the Spectrum: Promoting Health and Understanding / M. J. England, C. T. Liverman, A. M. Schultz. – The National Academies Press, 2012. – 537 р.
[2] World Health Organization – http://www.who.int/mediacentre/factsheets/fs999/ - May 2015р.
[3] Löscher, W. New avenues for antiepileptic drug discovery and development. / W. Löscher, H. Klitgaard, R. Twyman, D. Schmidt // Nat. Rev. Drug Discov. – 2013. – V.12 – P. 757–776.
[4] Shi-Ben W. Synthesis of 5-Alkoxythieno[2,3-e][1,2,4]triazolo[4,3-c]pyrimidine. Derivatives and Evaluation of Their Anticonvulsant Activities / W. Shi-Ben, P. Guang-Chun, Zh. Hong-Jian, Q. Zhe-Shan // J. Molecules – 2015. – V.22, – P. 6827-6843.
[5] Malik S. Synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: A hybrid pharmacophore approach / S. Malik, R.S. Bahare, S.A. Khan // Eur. J. Med. Chem. – 2013. – V.67 – P. 1–13.
[6] Shu B. Design, synthesis, and anticonvulsant activity evaluation of 4-(3-alkoxy-phenyl)-2,4-dihydro-[1,2,4]triazol-3-ones / B. Shu, Y. Zheng, S. Wang [et al.] // Arch. Pharm. – 2013. – V.346 – P. 127–133.
[7] Zhang C. B. Design and synthesis of 6-alkyoxyl[1,2,4] triazolo[1,5-a]quinazoline derivatives with anticonvulsant activity / C.B. Zhang, C.W. Yang, X.Q. Deng [et al.] // Med. Chem. Res. – 2012. – V.21, – P. 3294–3300.
[8] Deng X. Q. Synthesis and anticonvulsant activities of some triazolothiadiazole derivatives / X.Q. Deng, Z.Q. Dong, M.X. Song [et al.] // Arch. Pharm. – 2012. – V.345, – P. 565–573.
[9] Wei C. X. Synthesis and anticonvulsant activity of 1-formamide-triazolo[4,3-a]quinoline derivatives / C.X. Wei, X.Q. Deng, K.Y Chai [et al.] // Arch. Pharm. Res. J. – 2010. – V.33, – P. 655–662.
[10] Lagunin A. PASS: prediction of activity spectra for biologically active substances/ A. Lagunin, A. Stepanchikova, D. Filimonov, V. Poroikov // Bioinformatics. – 2000. - V. 16 (8), P. 747-748.
[11] Poroikov V. V. How to acquire new biological activities in old compounds by computer prediction / V. V. Poroikov, D. A. Filimonov // Journal of computer-aided molecular design – 2002. – Vol. 16 (11). – P. 819-824.
[12] Filimonov D. A. Prediction of the biological activity spectra of organic compounds using the PASS online web resource / D. A. Filimonov, A. A. Lagunin, T. A. Gloriozova, [et al.] // Chemistry of Heterocyclic Compounds. – 2014. – Vol. 50 (3). – P. 444-457.
[13] Saidov N. B. Pre-planning library of 3-mercapto-4-R-5-R1-4N-1,2,4-triazole purposefully to optimize the synthesis of biologically active substances / N. B. Saidov, V. A. Georgiyants // Proceedings of Shupyk national medical academy. – 2012. – Vol. 21 (4). – P.349-355.
[14] Saidov N. B. Synthesis, physico-chemical properties and prognosis of the pharmacological activity of 4-phenyl-5-(1,2,3-benzotriazolyl-1)-3-mercapto-1,2,4-triazole(4H) derivatives / N.B.Saidov, I.M.Kadamov, V.A.Georgiyants // Journal of organic and pharmaceutical chemistry. – 2012. – Т.10, Vol. 4 (40). – P. 25-28.
[15] Saidov N. B. Planning, Synthesis, and Pharmacological Activity of Alkyl Derivatives of 3-Mercapto-4-Phenyl-5-Arylaminomethyl-1,2,4-Triazole-(4H) / N. B. Saidov, I. M. Kadamov, V. A. Georgiyants, A. V. Taran // Pharmaceutical Chemistry Journal. - 2014. - Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 47, No. 11, pp. 11–15.
[16] http://www.pharmaexpert.ru/passonline/.
[17] Guidelines for conducting pre-clinical trials of medicinal products. Part one / A. N. Mironov, N. D. Bunyatyan, A. N. Vasilev [et al.] – Moscow: Grif&K, 2012. – 944 p.
[18] Golovenko M. Ya. Pre-clinical study of specific activity of potential anticonvulsants: Guidelines. / M.Ya. Golovenko, L.O. Gromov – Кiev: Avicena, 2003. – 26 p.
[19] Shtrygol’ S. Yu. Modulation of pharmacological effects at different salt modes: Monography / S. Yu. Shtrygol’– Kharkiv: Avista-VLT, 2007. – 360 p.
Author Information
  • Department of Pharmacology, National Pharmacy University, Kharkiv, Ukraine

  • Department of Pharmacology, National Pharmacy University, Kharkiv, Ukraine

  • Department of Pharmaceutical Chemistry, National Pharmacy University, Kharkiv, Ukraine

  • Department of Pharmaceutical Chemistry, National Pharmacy University, Kharkiv, Ukraine

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    Dmitryi Pavlovich Kavraiskyi, Sergey Yurievich Shtrygol', Victoria Akopovna Georgiyants, Narzullo Boboevich Saidov. (2017). Screening Investigation of Novel 1,2,4-Triazole-3-Thione Derivatives on Anticonvulsant Activity. International Journal of Pharmacy and Chemistry, 2(2), 47-51. https://doi.org/10.11648/j.ijpc.20160202.18

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    ACS Style

    Dmitryi Pavlovich Kavraiskyi; Sergey Yurievich Shtrygol'; Victoria Akopovna Georgiyants; Narzullo Boboevich Saidov. Screening Investigation of Novel 1,2,4-Triazole-3-Thione Derivatives on Anticonvulsant Activity. Int. J. Pharm. Chem. 2017, 2(2), 47-51. doi: 10.11648/j.ijpc.20160202.18

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    AMA Style

    Dmitryi Pavlovich Kavraiskyi, Sergey Yurievich Shtrygol', Victoria Akopovna Georgiyants, Narzullo Boboevich Saidov. Screening Investigation of Novel 1,2,4-Triazole-3-Thione Derivatives on Anticonvulsant Activity. Int J Pharm Chem. 2017;2(2):47-51. doi: 10.11648/j.ijpc.20160202.18

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  • @article{10.11648/j.ijpc.20160202.18,
      author = {Dmitryi Pavlovich Kavraiskyi and Sergey Yurievich Shtrygol' and Victoria Akopovna Georgiyants and Narzullo Boboevich Saidov},
      title = {Screening Investigation of Novel 1,2,4-Triazole-3-Thione Derivatives on Anticonvulsant Activity},
      journal = {International Journal of Pharmacy and Chemistry},
      volume = {2},
      number = {2},
      pages = {47-51},
      doi = {10.11648/j.ijpc.20160202.18},
      url = {https://doi.org/10.11648/j.ijpc.20160202.18},
      eprint = {https://download.sciencepg.com/pdf/10.11648.j.ijpc.20160202.18},
      abstract = {1,2,4-triazole and its derivatives are present in many biologically active aromatic compounds that have different biological properties and clinical applications including anticonvulsant activity. The number of studies in this direction is increasing. Therefore, based on the results of previous computer predictions, 8 novel 1,2,4-triazole-3-thione derivatives have been synthesized in the Department of Pharmaceutical Chemistry at the National Pharmacy University of Ukraine. The screening test of novel 1,2,4-triazole-3-thione derivatives on anticonvulsant activity in PTZ-induced seizures was conducted on mice. Among test substances revealed were those, which in the dose of 100 mg/kg showed moderate anticonvulsive effect and which were non-inferior to "reference drug" sodium valproate by some parameters. Screening results have confirmed the reasonability of in-depth anticonvulsive activity study of substances-leaders, pharmacological study of their mechanism of action, spectrum of anticonvulsant activity, concurrent types of pharmacological activity, dose-dependence of effect and safety.},
     year = {2017}
    }
    

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  • TY  - JOUR
    T1  - Screening Investigation of Novel 1,2,4-Triazole-3-Thione Derivatives on Anticonvulsant Activity
    AU  - Dmitryi Pavlovich Kavraiskyi
    AU  - Sergey Yurievich Shtrygol'
    AU  - Victoria Akopovna Georgiyants
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    JF  - International Journal of Pharmacy and Chemistry
    JO  - International Journal of Pharmacy and Chemistry
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    AB  - 1,2,4-triazole and its derivatives are present in many biologically active aromatic compounds that have different biological properties and clinical applications including anticonvulsant activity. The number of studies in this direction is increasing. Therefore, based on the results of previous computer predictions, 8 novel 1,2,4-triazole-3-thione derivatives have been synthesized in the Department of Pharmaceutical Chemistry at the National Pharmacy University of Ukraine. The screening test of novel 1,2,4-triazole-3-thione derivatives on anticonvulsant activity in PTZ-induced seizures was conducted on mice. Among test substances revealed were those, which in the dose of 100 mg/kg showed moderate anticonvulsive effect and which were non-inferior to "reference drug" sodium valproate by some parameters. Screening results have confirmed the reasonability of in-depth anticonvulsive activity study of substances-leaders, pharmacological study of their mechanism of action, spectrum of anticonvulsant activity, concurrent types of pharmacological activity, dose-dependence of effect and safety.
    VL  - 2
    IS  - 2
    ER  - 

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