Charbe Nb, M. Ap, Shende Sg
Jun 30, 2010
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Abstract
Meta nitro benzoic acid has been reduced to 3-aminocyclohexa-1,5-diene-1-carboxylic acid with three different Birch like reduction condition (Method I, II, III) to 3-aminocyclohexa-1,4-diene-1-carboxylic acid. 3-aminocyclohexa-1,4-diene-1-carboxylic acid is found to be structurally more super impossible on gama-amino butyric acid (GABA) and hence the synthesized compounds was tested for the CNS depressant and muscle relaxant activities. A series of new 3-(5-substituted phenyl-1,3,4-thiadiazole-2-yl)-2- styryl 5,8-dihydroquinazoline-4 (3H)-ones were synthesized and evaluated for anticonvulsant, sedative- hypnotic and CNS depression activities. Various derivatives of 3-(5-substituted phenyl-1,3,4-thiadiazole-2- yl)-2-styryl 5,8-dihydroquinazoline-4 (3H)-ones were examined in the maximal electroshock (MES) induced seizures and subcutaneous pentylenetetrazole (scPTZ) induced seizure models in mice. Rotorod method was employed to determine the neurotoxicity. Out of 9 compounds only 3 compounds showed anticonvulsant activity in one or more test models. All except compound (a) exhibited significant sedative- hypnotic activity via actophotometer screen. Forced swim pool method to determine CNS depressant activity resulted in some potent compounds. It can be concluded that synthesized compounds exhibited better sedative-hypnotic and CNS depressant activities than anticonvulsant activity.