Title: Anticonvulsant Activity of A Novel Series of 2,5-Disubstituted 1,3,4-Oxadiazoles: Semicarbazones Based Pharmacophoric Model Studies
Volume: 6
Issue: 6
Author(s): Harish Rajak, Ravichandran Veerasamy, Pradeep Singour, Murli Dhar Kharya and Pradeep Mishra
Affiliation:
Keywords:
1,3,4-Oxadiazoles, Semicarbazones, Anticonvulsant activity, Neurotoxicity
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.
