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Published on:June 2021
Indian Journal of Pharmaceutical Education and Research, 2021; 55(2s):s595-s604
Analysis | doi:10.5530/ijper.55.2s.132

Synthesis and Anticonvulsant Evaluation of 3-(5-(4-substitutedphenyl)-4,5-dihydro-1H-pyrazol- 3-ylamino)-2-(2-methylphenyl)quinazolin-4(3H)-one Derivatives


Authors and affiliation (s):

Sachin Kumar1, Keshari Kishore Jha2, Rati Kailash Prasad Tripathi3, Nishant Kumar4, Anurag Chaudhary4,

1IIMT College of Medical Sciences, IIMT University, Meerut, Uttar Pradesh, INDIA.

2College of Pharmacy, Teerthanker Mahaveer College of Pharmacy, Teerthanker Mahaveer University, Moradabad, Uttar Pradesh, INDIA.

3Department of Pharmaceutical Chemistry, Parul Institute of Pharmacy, Vadodara, Gujarat, INDIA.

4Department of Pharmaceutical Technology, Meerut Institute of Engineering and Technology, Meerut, Uttar Pradesh, INDIA.

Abstract:

Epilepsy arise due to discharge of electric current in CNS and it is Characterized by repeated seizure because of different factors like social, neurological and environmental or it may be due to genetic or non-genetic. A large number of AED’s used to treat epilepsy but all these shows drug resistance and side effects, so research interest continue to find out novel antiepileptic drugs with higher efficiency and less toxicity.A novel series of 3-(5-(4-substitutedphenyl)-4,5-dihydro-1H-pyrazole-3-ylamino)-2-(2-methylphenyl) quinazole4(3H)-one was developed, synthesized and evaluated for anticonvulsant activity using two pharmacological models, maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) models. Spectral data and elemental analysis were used to validate the structure of the synthetic compounds. Synthesized substances have also been tested for their neurotoxicity by rotary apparatus. Both compounds display strong anticonvulsant and neurotoxic activity. 3-(5-(4-fluorophenyl)-4,5-dihydro- 1H-pyrazole-3-ylamino)-2-(2-methylphenyl)quinazole-4(3H)-one, 8(v) was found to be the most successful in maximal electroshock seizure (percentage protection = 73.63 at 150 mg/kg) and subcutaneous pentylenetetrazole induced convulsion model (percentage protection = 75.59 at 150 mg/kg) models and was found to be non-neurotoxic.

Key words: AED’s, Qinazolin-4-(3H)-one, Anticonvulsant, MES, scPTZ, Neurotoxicity.

 




 

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The Official Journal of Association of Pharmaceutical Teachers of India (APTI)
(Registered under Registration of Societies Act XXI of 1860 No. 122 of 1966-1967, Lucknow)

Indian Journal of Pharmaceutical Education and Research (IJPER) [ISSN-0019-5464] is the official journal of Association of Pharmaceutical Teachers of India (APTI) and is being published since 1967.

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