Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Anticonvulsant Activity of A Novel Series of 2,5-Disubstituted 1,3,4-Oxadiazoles: Semicarbazones Based Pharmacophoric Model Studies

Author(s): Harish Rajak, Ravichandran Veerasamy, Pradeep Singour, Murli Dhar Kharya, Pradeep Mishra.

Abstract:

In searching for better anticonvulsant drug and the importance of semicarbazones and 2,5-disubstituted 1,3,4- oxadiazoles as anticonvulsant pharmacophore, a series of novel substituted semicarbazones were designed, synthesized and evaluated for their anticonvulsant activity. Among all the synthesized compounds, N1-(5-{2-[(2,6- dichlorophenyl)amino]benzyl}-1,3,4-oxadiazol-2-yl)-N4-[1-(4-hydroxyphenyl)(phenyl) methanone]-semicarbazone 12 emerged out as the most potent compound, showing considerable activity in maximal electroshock seizure (at 100 mg/kg after 0.5 h and at 300 mg/kg after 4.0 h) and subcutaneous pentylenetrtrazole model (at 300 mg/kg after 4.0 h) without any neurotoxicity (up to 300 mg/kg after 4.0 h). The results of the present study validated that the pharmacophore model with four binding sites is essential for anticonvulsant activity.

Keywords: 1,3,4-Oxadiazoles, Semicarbazones, Anticonvulsant activity, Neurotoxicity

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Article Details

VOLUME: 6
ISSUE: 6
Year: 2009
Page: [456 - 463]
Pages: 8
DOI: 10.2174/157018009789057571
Price: $58