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Design and Development of novel anticonvulsants
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KOMAL TRIVEDI, DHARTI GAJERA
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| Abstract:
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The anticonvulsant action of pyrazole moiety is ascribed to its unique properties of being a two-electron donor system and ability to act as a constrained pharmacophore at the receptor site. It is observe that anticonvulsant drugs having diazine nucleus which give inhibitory effect. Pyrazole having diazine nucleus which contain hydrazide fragment which is observed in number of the anticonvulsants. A several number of novel 4-methoxy-2-[5-(aryl/substituted aryl)-1H pyrazole-3yl] phenol have been synthesized by the reaction of 1-(2-hydroxy-4-methoxy phenyl)-3-(4-substituted phenyl) propane-1, 3-dione and appropriate unsubstituted hydrazine in ethanol. 1-(2-hydroxy-4-methoxy phenyl)-3-(4-substituted phenyl) propane-1, 3-dione were synthesized by the 4-methoxy phenyl substituted benzoate which were synthesized by the reaction of 2-hydroxy acetophenone with appropriate unsubstituted and substituted benzoic acid. The synthesized compounds were confirmed by melting point and TLC and their structure was established by various analytical techniques such as IR and 1HNMR spectral studies. The anti-convulsant screening results reveal that among all the compounds screened, compounds KBPR-3.1 and KBPR-3.3 showed moderate anti-convulsant activity, while compounds KBPR-3.2 and KBPR-3.5,displayed good anti-convulsant activity (% protection at concentration of 0.1ml/20mg) when compared with Phenytoin used as standard.
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Keywords: pyrazoles, hydrazines, cyclization, diaryl pyrazoles,anticonvulsants
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