Anticonvulsant appraisal of benzylideneacetophenone analogues in Swiss mice

Main Article Content

Azibanasamesa D.C Owaba
James O. Kemelayefa
Oyeintonbra Miediegha


Background: Diketones and α,β-unsaturated ketone are useful intermediates for the synthesis of antiepileptic moieties. Epilepsy is a neurological disorder that affects about fififty million people worldwide. The aim of the study was to assess benzylideneacetophenone analogues for their potential antiepileptic effects in mice.

Methods: The compounds used in the pharmacological assay which include; 4-Dimethylaminochalcone (A), 1(4-Nitrophenyl) – 3 (ϒ -benzopyranoyl)-2-propen – 1-one (B), 1(4' –Nitrophenyl) – 3 (1,3-benzodioxolyl) 2 – propen – 1 – one (C), 1-Phenyl-3- (benzodioxolyl) – 2 –propen – 1-one (D), 4-Chlorochalcone (E), 4'-Nitro-4-dimethylaminochalcone (F) 4'-Nitro-4-methoxychalcone (G), were assayed using three models; Strychnine, Pentylenetetrazole (PTZ) and Maximal Electroshock (MES). The samples were given at 500, 1000 and 1500 mg/kg while standard drug diazepam and distilled water were given at 5 mg and 10 ml/kg intraperitoneal respectively. Convulsion inducing agents (Strychnine 2 mg/kg and PTZ, 100 mg/kg) were administered intraperitoneal 1hour after the administration of test samples while MES model electroconvulsive shock was applied using electroconvulsive machine. 

Results: The samples (A-G) showed significant (P<0.03, 0.003, 0.0007 and 0.0001) effect in delaying onset of seizure compared to control in strychnine model, while in PTZ model samples (A-F) evaluated at 500,1000 and 1500 mg/kg are equipotent at all the doses by signifificantly (P<0.0001) and sample G (P<0.0007) reduced the onset of seizure compared to control. However in MES model samples (A-F and G) evaluated at 500, 1000 and 1500 mg/kg are equipotent at all the doses by significantly (P<0.0001; 0.0007), reduced the duration of seizure compared to control respectively. 

Conclusion: Benzylideneacetophenone analogues showed various effects in control of seizure in all the models used.This effect is due to delayed onset and reduction of seizure duration. The samples could act by stimulating the glycine, Gamma Aminobutyric acid (GABA) receptor, inhibition of GABAAminotransferase and prolong inactivation of sodium ion channel.

Article Details

How to Cite
Owaba, A. D. ., Kemelayefa, J. O. ., & Miediegha, O. . (2022). Anticonvulsant appraisal of benzylideneacetophenone analogues in Swiss mice: The Nigerian Journal of Pharmacy, 56(2). Retrieved from


Hegde, K., Thakker, S. P., Joshi, A. B., Shastry, C. S. and Chandr a shekha r, K. S. (2009). Anticonvulsant activity of Carisa carandas Linn root extract in experimental mice. Tropical Journal of Pharmaceutical Research, 8(2): 117-125.

Ataee, R., Falahati, A., Ebrahimzadeh, M. A., Shokrzadeh, M. (2016). Anticonvulsant activities of Sambucusnigra. European Review for Medical and Pharmacological Sciences, 20, 3123-3126.

Ahmad, A. H. and Amabeoku, G. J. (2013). Involvement of Gamma Aminobutyric acid in the anticonvulsant effect of the leaf methanol extract of Ruta graveolens L. (Rutaceae) in mice. International Journal of Pharmacology, 9(2): 134 - 142. Doi:

Ojong, L. J., Abdou, J. P., Kandeda, A. K., Yaya, A. J. G., Tchamgoue, A. D., Tchokouaha, L. R. Y., Nkantchoua, N. G. C., Agbor, G. A., Moyou, R. S., and Ngo, E. B. (2016). Anticonvulsant and in vitro antioxidant activities of Momordica cissoides L. (Curcurbitaceae). Journal of Applied Pharmaceutical Science, 6(04): 117-123. DOI:

Okunne, T. C. (2019). Antiepileptic agents. In: Ozolua, R.I, Bafor, E.E. A Handbook of Techniques in Experimental Pharmacology,

Mindex Publishing Company Limited,Benin, Nigeria, 189-195.

Owaba, A. D. C., Oyeintonbra, M. and Raji, R. O. (2020). Chalcones as synthon for heterocyclic compounds- A review. International Journal of Current Research, 12(09): 13672-13681. Doi:

Krishna , G. O. (2017). Eva lua tion of anticonvulsant and anxiolytic activity of methanolic extract of Syzgium aqueum (Brum f),

Department of Pharmacology, JKKMMRF'S College of Pharmacy, Tamil Nadu. 14-15p.

Moto, F. C. O., Mbafor, J. T., Bum, E. N., Kouemou, N., Kandeda, A. K., Talla, E., Dimo, T., Rakotonirira, A. and Rakotonirira, S. V. (2011). Evaluation of the sedative and anticonvulsant properties of three Camerounian Plants. African Journal of Complimentary and Alternative Medicine, 8(S): 181 - 190. DOI:

Manu, G., Padmanabha, S. T., Chandrakantha, T. and Ravishankar, M. (2017). Evaluation of anticonvulsant activity of ethanolic extracts of Leaves of Ocimum sanctum (Tulsi) in Albino rats. National Journal of Physiology, Pharmacy and Pharmacology, 7(7): 761 - 764. Doi: 10.5455/njppp.2017.7.0308122032017

Owaba, A. D. C., Kemelayefa. O. J. and Eboh, A. S. (2021). Synthesis of benzylideneacetophenone and anti-seizure evaluation. Journal of Chemistry Studies, 5(1): 38-43.

Owaba, A. D. C., Etim, E. I., Johnson, E. C. (2022). Comparative haematological Effect of Seed and Stem Bark Extracts of Carapa Procera D.C Meliaceae in Male Rodents. The Journal of Phytopharmacology, 11(1): 137-141. DOI: doi.10.31254/phyto.2022.11116

Akubue, P. I. (2005). Drug Therapy in Epilepsy In: Akubue PI, Textbbook of Pharmacology, Africana First Publisher Limited,

Onitsha Nigeria, 394-407.

Hansch, C. and Kerley, R. (1970). Role of the benzyl moiety in biochemical and pharmacological processes. Journal of Medicinal Chemistry. 13 (5): 957 - 64. doi: 10.1021/jm00299a036.

Razdan, B. (2010). Medicinal Chemistry. CBS Publishers and Distributors Pvt Ltd, New Delhi, India, Pp 201-206, 469-447.

Abubakar, U. S., Danmallam, U. H., Ibrahim, H. and Maiha, B. B. (2020). Anticonvulsant activity of aqueous stem bark extract of Securi dacalong ipedunculata Fresen (Polygalaceae). Dutse Journal of Pure and Applied Sciences, 6(2): 277-286.