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Rajak H.,Guru Ghasidas University | Deshmukh R.,Guru Ghasidas University | Veerasamy R.,AIMST University | Sharma A.K.,Pharmacology Research Laboratory | And 2 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2010

A series of novel N 1-{5-[(naphthalene-2-yloxy)methyl]-1,3,4-oxadiazol-2-yl}-N 4-(4-substitutedbenzaldehyde)-semicarbazone, N 1-{5-[(naphthalene-2-yloxy)methyl]-1,3,4-oxadiazol-2-yl}-N 4-[1-(4-substitutedphenyl)ethanone]-semicarbazone and N 1-{5-[(naphthalene-2-yloxy)methyl]-1,3,4-oxadiazol-2-yl}-N 4-[1-(4-substitutedphenyl) (phenyl) methanone]-semicarbazone were designed and synthesized on the basis of semicarbazone based pharmacophoric model to meet the structural requirements necessary for anticonvulsant activity. The anticonvulsant activities of the compounds were investigated using maximal electroshock seizure (MES), subcutaneous pentylenetrtrazole (scPTZ) and subcutaneous strychnine (scSTY) models. Some of the selected active compounds were subjected to GABA assay to confirm their mode of action. The efforts were also made to establish structure activity relationships among synthesized compounds. The results of the present studying validated that the pharmacophoric model with four binding sites is essential for anticonvulsant activity. © 2010 Elsevier Ltd. All rights reserved. Source


Rajak H.,Guru Ghasidas University | Singour P.,VNS Institute of Pharmacy | Kharya M.D.,Dr Hari Singh Gour University | Mishra P.,GLA Institute of Pharmaceutical science and Research
Chemical Biology and Drug Design | Year: 2011

In search for a 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. The chemical structures of the synthesized molecules were confirmed by elemental and spectral (IR, 1H NMR, 13C NMR and MS) analysis. The anticonvulsant activities of the compounds were investigated using maximal electroshock seizure and subcutaneous pentylenetetrazole (scPTZ) models. Efforts were also made to establish structure-activity relationships among synthesized compounds. The results of the present study validated that the pharmacophore model with four binding sites is essential for anticonvulsant activity. © 2011 John Wiley & Sons A/S. Source


Rajak H.,Guru Ghasidas University | Aggarwal N.,Guru Ghasidas University | Kashaw S.,Guru Ghasidas University | Kashaw S.,Dr Hari Singh Gour University | And 4 more authors.
Journal of the Korean Chemical Society | Year: 2010

The synthesis of novel 2,5-disubstituted 1,3,4-thiadiazoles and their anticonvulsant activity was analyzed. The synthesis of 1-[5-{(2-methyl-1H- benzimidazol-1-yl)methyl}-1,3,4-thiadiazol-2-yl]-urea involved the dissolution of 5-[(2-methyl-1H-benzimidazol-1-yl)-methyl]-1,3,4-thiadiazol-2-amine in 10 ~ 30 mL of glacial acetic acid diluted to 50 mL with distilled water and to the equimolar (0.01 mol) quantity of sodium cyanate in 20 ~ 30 mL of warm water was added. The precipitates obtained were collected by filtration, washed with cold water and recrystallized from 90% aqueous ethanol. The synthesis of N-[5-(1H-indol-3-yl-methyl)-1,3,4-thiadiazol-2-yl]-hydrazinecarboxamide involved the dissolution of 1-[5-{(2-methyl-1H-benzimidazol-1-yl)methyl}-1,3,4- thiadiazol-2-yl]-urea in 30 ~ 40 mL and to the mixture equimolar solution of hydrazine hydrate in 5 mL of water was added. The product was filtered and recrystallized from 90% aqueous ethanol. It was reported that majority of the compounds exhibited anticonvulsant activity. Source

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