Synthesis and Structure-Activity Relationship on Anticonvulsant Aryl Semicarbazones

Title: Synthesis and Structure-Activity Relationship on Anticonvulsant Aryl Semicarbazones

Volume: 2 Issue: 1

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

Affiliation:

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

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.

Cite this article as:

Sriram D., Stables P. J., Thirumurugan R., Induja S., Ragavendran V. J. and Yogeeswari P., Synthesis and Structure-Activity Relationship on Anticonvulsant Aryl Semicarbazones, Medicinal Chemistry 2006; 2 (1) . https://dx.doi.org/10.2174/157340606775197778