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ABSTRACT
| Title |
: |
SYNTHESIS AND BIOLOGICAL EVALUTION OF 3-CHLORO 2-METHYL PHENYL CARBAMOYL SUBSTITUTED SEMICARBAZONE DERIVATIVES AS POTENTIAL ANTICONVULSANT AGENTS |
| Authors |
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Laxmi Banjare, Yogesh Vaishnav, Devendra Thakur, Pranita Kashyap |
| Keywords |
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3- Chloro 2-methyl phenyl carbamoyl substituted semicarbazone derivatives ,Neurotoxicity ,Electroshock ,Phentylenetetrazole ,Anticonvulsant activity |
| Issue Date |
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January 2012 |
| Abstract |
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A series of 3- chloro 2- methyl phenyl carbamoyl substituted semicarbazones (4-21) was synthesized and evaluated for anticonvulsant and CNS activities. The anticonvulsant activity of the synthesized compounds was established after intraperitoneal administration in three seizure models in mice which include maximal electroshock seizure, subcutaneous pentylenetetrazole, and subcutaneous strychnine-induced seizure screens. All the test compounds were administered at doses of 30, 100, and 300 mg/kg body weight and the anticonvulsant activity was noted at 0.5 and 4 h time intervals after the drug administration . . Aryl semicarbazides have also been reported to display excellent anticonvulsant activity in mice and rats . In terms of interaction at the binding site, as proposed previously by Dimmock et al. the pharma-cophoric elements were thought to be a lipophilic aryl ring and hydrogen bonding semicarbazone moiety. The attach- ment of a second aryl ring designated as the distal ring to the proximal aryl ring to increase the van der Waal’s bonding at the binding site and to increase potency have also been reported. Substitutions in the aryl ring by halogens have been found to increase potency in the MES screen . |
| Page(s) |
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226-240 |
| ISSN |
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0975-9492 |
| Source |
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Vol. 3, No.1 |
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