SYNTHESIS, CHARACTERIZATION AND ANTICONVULSANT ACTIVITY OF SOME PYRAZOLE DERIVATIVES

Anandarajagopal Kalusalingam, Illavarasu Arumugamb, Rajamanickam Velayutham, U. Natarajan, Anbu Jeba Sunilson Johnsamuela, Proom Promwichita
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引用次数: 3

Abstract

A several number of novel 4-(aryl/substituted aryl)-1-(unsubstituted/aryl/substituted aryl)-3-phenyl-1H-pyrazoles have been synthesized by the reaction of 1-substituted phenyl-3-phenyl-2,3-dibromo prop-1-ones and appropriate unsubstituted and substituted hydrazine in ethanol. 1-substituted phenyl-3-phenyl-2,3-dibromo prop-1-ones were synthesized by the bromination of 1-substituted phenyl-3-phenyl-prop-2-en-1-ones which were synthesized by the reaction of acetophenone with appropriate unsubstituted and substituted aromatic aldehyde. 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 anticonvulsant activity of the synthesized compounds has indicated that all the compounds significantly reduce the electro shock induced convulsions, compared to phenytoin. The pharmacological evaluation may be concluded that the replacement of 1H position of pyrazole with phenyl and substituted phenyl increases the anticonvulsant activity.
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吡唑衍生物的合成、表征及抗惊厥活性
以1-取代苯基-3-苯基-2,3-二溴丙烷为原料,在乙醇中与适当的未取代和取代肼反应,合成了若干新型的4-(芳基/取代芳基)-1-(未取代/芳基/取代芳基)-3-苯基- 1h -吡唑。以苯乙酮与适当的未取代和取代芳香醛反应合成的1-取代苯基-3-苯基-2-苯基-2-烯-1为原料,通过溴化反应合成1-取代苯基-3-苯基-2,3-二溴丙烷-1。通过熔点和薄层色谱对合成的化合物进行了确证,并通过IR和1HNMR光谱等多种分析技术确定了化合物的结构。合成化合物的抗惊厥活性表明,与苯妥英相比,所有化合物都能显著减少电休克引起的惊厥。药理学评价表明,用苯基和取代苯基取代吡唑的1H位增加了抗惊厥活性。
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