Design, Synthesis and In-Vivo Anticonvulsant Evaluation Of 5-[(E)- (3,4,5-Trimethoxybenzylidene) Amino]-1,3,4-Thiadiazole-2-Thiol

Authors

  • Aliyu, A. Ahmadu Bello University, Zaria
  • Idris, A. Y. Ahmadu Bello University, Zaria
  • Musa, A. M. Ahmadu Bello University, Zaria
  • Hamza, A. N. Ahmadu Bello University, Zaria
  • Ahmadu, J. O. Ahmadu Bello University, Zaria
  • Shehu, A. Ahmadu Bello University, Zaria
  • Salisu, A. Federal University Gusau

Keywords:

Anticonvulsant, 1,3,4-thiadiazole-2-thiol, lipophylicity

Abstract

5-[(E)-(3,4,5-trimethoxybenzylidene)amino]-1,3,4-thiadiazole-2-thiol was designed based on ADME prediction and a proposed pharmacophore model, and synthesized by condensation reaction.The structure of the compound was established by means of FTIR, UV-Visible, 1H and 13C nuclear magnetic resonance spectroscopy, mass spectroscopy and elemental analyses. The compound was evaluated for its anticonvulsant activity using maximal electroshock (MES) and subcutaneous pentylene tetrazole (PTZ) test models and its acute toxicity and neurotoxicity studies were determined. The compound showed no sign of neurotoxicity, and it exhibits significant protection, showing potent activity in both test models. The present findings suggest that 5-[(E)-(3,4,5-
trimethoxybenzylidene)amino]-1,3,4-thiadiazole-2-thiol possesses anticonvulsant activity and is a candidate for further optimization and evaluation. Furthermore, the results evidenced the significance of Schiff bases in disubstituted 1,3,4-thiadiazole compounds by improving lipophylicity and thus, showing better anticonvulsant activity.

Author Biographies

Aliyu, A., Ahmadu Bello University, Zaria

Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ahmadu Bello University, Zaria.

Idris, A. Y., Ahmadu Bello University, Zaria

Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ahmadu Bello University, Zaria

Musa, A. M., Ahmadu Bello University, Zaria

Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ahmadu Bello University, Zaria.

Hamza, A. N., Ahmadu Bello University, Zaria

Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ahmadu Bello University, Zaria.

Ahmadu, J. O., Ahmadu Bello University, Zaria

Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ahmadu Bello University, Zaria.

Shehu, A., Ahmadu Bello University, Zaria

Department of Pharmacology and Therapeutics, Faculty of Pharmaceutical Sciences, Ahmadu Bello University, Zaria

Salisu, A., Federal University Gusau

Department of Chemistry, Federal University Gusau.

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Published

2021-07-26

How to Cite

Aliyu, A., Idris, A. Y., Musa, A. M., Hamza, A. N., Ahmadu, J. O., Shehu, A., & Salisu, A. (2021). Design, Synthesis and In-Vivo Anticonvulsant Evaluation Of 5-[(E)- (3,4,5-Trimethoxybenzylidene) Amino]-1,3,4-Thiadiazole-2-Thiol. International Journal of Science for Global Sustainability, 7(2), 8. Retrieved from https://fugus-ijsgs.com.ng/index.php/ijsgs/article/view/35

Issue

Vol. 7 No. 2 (2021): INTERNATIONAL JOURNAL OF SCIENCE FOR GLOBAL SUSTAINABILITY (IJSGS)

Section

Articles