Abstract

In the present study, a series of 4-(4-substituted aryl) semicarbazones were synthesized from substituted anilines and subsequently evaluated for their anticonvulsant activities. The anticonvulsant activities were established by the anticonvulsant drug development (ADD) programme NIH, USA using experimental animal, adult male FCM mice (20–25 g) and adult Sprague-Dawley rats (100–150 g) and screened against electroshock seizure, subcutaneous metrazole and minimal neurotoxicity tests in mice. Compound 7 was found equipotent to carbamazepine in both MES and ScPTZ tests. This study has highlighted the importance of distal alkyl chain which influences the anticonvulsant activity.

Highlights

  • In the present study, a series of 4-(4-substituted aryl) semicarbazones were synthesized from substituted anilines and subsequently evaluated for their anticonvulsant activities

  • Here we demonstrate the lipophilic aryl ring substitution in semicarbazones along with nitro

  • The anticonvulsant activities were established by the anticonvulsant drug development (ADD)

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Summary

Introduction

A series of 4-(4-substituted aryl) semicarbazones were synthesized from substituted anilines and subsequently evaluated for their anticonvulsant activities. The lipophilic aryl ring with chloro, bromo or nitro groups have been found to be essential for anticonvulsant activity. (%) 65; Rf 0.63; UV (EtOH, Band λmax nm) 231, 373, 379; IR (KBr, cm-1) 3365 (Ar-NH), 1635 (C=O), 1475 (Ar-NO ), 845 (Ar-H); 1H NMR (DMSO d -TMS, ppm) 5.9 (s, 1H, Ar-NH), 3.4-3.7 (m, 16H, camphor ring), 6.4-6.7 (m, 4H, nitrophenyl ring), 7.6-8.0(d, 2H,NH).

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