Synthesis and Structure-Activity Relationship on Anticonvulsant Aryl Semicarbazones

Author(s): D. Sriram, J. P. Stables, R. Thirumurugan, S. Induja, J. V. Ragavendran, P. Yogeeswari

Journal Name: Medicinal Chemistry

Volume 2 , Issue 1 , 2006

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Abstract:

Seven series of various substituted aryl semicarbazones were synthesized and evaluated for anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) induced seizure threshold tests. A comprehensive structure-activity relationship was derived comparing the substituents on the aryl ring and in the carbimino terminal. Generally the order of activity was 4-F > 2-Br = 3-Br = 4-Cl > 4-CH3 > 4-Br > 3-Cl > 3- CH3 with respect to the primary aryl group. Most of the compounds exhibited activity both in the MES and scPTZ screens. The 4-fluorophenyl substituted semicarbazones (5a-5y) emerged as the most potent compounds exhibiting anticonvulsant activity in mouse intraperitoneal (i.p.) and rat per oral (p.o.) MES, scPTZ and psychomotor seizure (6 Hz) screens.

Keywords: anticonvulsant activity, Aryl semicarbazones, 4-fluorophenyl, maximal electroshock seizure

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Article Details

VOLUME: 2
ISSUE: 1
Year: 2006
Page: [55 - 62]
Pages: 8
DOI: 10.2174/157340606775197778

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