Introduction
Epilepsy is a central nervous system (CNS) malfunction that
leads either to generalized hyperactivity involving essentially
all parts of the brain or to hyperactivity of only a portion of the
brain (Guyton, 1976). epilepsy is a collective term that includes
over 40 different types of human seizures disorders. Approx
1% of the world population at any one time (>50 million people
worldwide) is afflicted with these serious neurological
disorders. Although the current drug provides adequate seizure
control in many patients, it is roughly estimated that up to 28-
30% of patients are poorly treated with the available
antiepileptic drugs (AEDs). Moreover, many (AEDs) have
serious side effects and lifelong medication may be
required. Conventional antiepileptic drugs (AEDs).
Phenobarbital, primidone, phenytoin, carbamazepine,
ethosuximide, and benzodiazepines, are widely used but
exhibit an unfavorable side effect profile and failure to
adequately control seizures in the recent year new drugs
(Oxcarbazepine, Lamotrigine, Topiramate, Gabapentin,
Zonisamide, Tiagabine, Fosphenytoin, Vigabatrine &
felbamate) have been added to the list of therapeutic agents
against epilepsy (Mccormick and Contreras, 2001).
However, there is a significant group of patients (up to
30%) who are resistant to the available anti-epileptic drugs.
The long-established AED control seizures in 50% of
people developing partial seizures and in 60-70% of those
developing generalized seizures (Meador, 2003).
In the 1960s, research in antiepileptic drug development
Screening of some Semicarbazones as anticonvulsant agent
Ajay Kumar Garg *, Ranjan Kumar Singh , Khushboo Srimali , Saurabh K. Sinha
1 2 3 4
, Vivek Jain
4
1
Department of Pharmaceutical Chemistry, Shekhawati Institute of Pharmacy, Rajasthan, India
2
Department of Pharmacology, Shekhawati Institute of Pharmacy, Rajasthan, India
3
Department of Pharmaceutical Chemistry, Mahatma Gandhi College of Pharmacy, Rajasthan, India
4
Department of Pharmaceutical Sciences, Mohanlal Sukhadia University, Udaipur, Rajasthan-313001, India
* Corresponding Author: Address for
Ajay Kumar Garg
Department of Pharmaceutical Chemistry,
Shekhawati Institute of Pharmacy, Rajasthan, India
Email: ajay.pharma3006@gmail.com
Abstract
Objective: The principal objective of the present investigation was the preparation of several analogs to further
evaluate the binding site hypothesis. Aryl semicarbazides have also been reported to display excellent anticonvulsant
activity in mice and rats. In this project, the synthesis of semicarbazone derivatives was Matearial and Methods:
carried out. All molecules were synthesized using the common starting material –aniline. In all compounds, an
intermediate was first formed by substituted phenyl urea using substituted aniline and potassium cyanate, and then it
was hydrolyzed to get substituted phenyl semicarbazide, which was directly coupled with ketones. All the
synthesized compounds were biologically screened for their anticonvulsant activity by the MES method. Results:
Standard error mean was calculated concerning standard and control drug, Phenytoin sodium (25mg/kg.) and
DMSO. The synthesized semicarbazone was characterized by using IR Spectroscopy. One another representative
molecule compound was characterized using H NMR Spectroscopy. It can be concluded that designed
1
Conclusion:
semicarbazones were synthesized and characterized successfully. After synthesis of designed semicarbazones
compounds were evaluated for anticonvulsant activity. Finally, two compounds have shown better activity in
comparison to the other molecules.
Keywords: Semicarbazone, MES, SEM, anticonvulsant activity, IR, NMR spectroscopy
Research Article
Received: 17 January 2022 Revised: 7 February 2022 Accepted: 26 February 2022
www.apjonline.in
DOI: https://doi.org/10.31024/apj.2022.7.1.2
2456-1436/Copyright © 2022, N.S. Memorial Scientific Research and Education Society. This is an open access article under the CC BY-
NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
Advance Pharmaceutical Journal 2022; 7(1):16-22 16