Synthesis and biological activity of some pyrimidine derivatives

Kikkeri N. Mohana , Basavapatna N. Prasanna Kumar , Lingappa Mallesha
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引用次数: 58

Abstract

Objectives

To synthesize a variety of pyrimidine analogs, 3, 4, 5, 6(a–d), 7(a–d) and their anticonvulsant and antioxidant activity was determined.

Methods

Using 5-bromo-2,4-dichloropyrimidine and hydrazine hydrate, new compounds were synthesized. The structures of all the new compounds are established on the basis of FT-IR, 1H NMR and mass spectral data. Anticonvulsant study was done by MES seizure model and rotorod method was employed to determine the neurotoxicity. Antioxidant activity was done by DPPH method.

Results

All the compounds were synthesized in good yield. Among the new compounds, 6c and 7c are found to be most potent and showed no neurotoxicity. All the compounds showed DPPH radical scavenging activity, where compounds 7b, 7a and 6b were the best radical scavengers.

Conclusions

The results obtained justify the usage of these compounds from their promising anticonvulsant and antioxidant activity. Therefore, the nature of groups is very important for anticonvulsant activity in MES model.

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一些嘧啶衍生物的合成及其生物活性
目的合成多种嘧啶类似物3、4、5、6(a - d)、7(a - d)并测定其抗惊厥和抗氧化活性。方法以5-溴-2,4-二氯嘧啶和水合肼为原料合成新化合物。所有新化合物的结构都是根据FT-IR, 1H NMR和质谱数据确定的。采用MES发作模型进行抗惊厥研究,采用旋流法测定神经毒性。DPPH法测定其抗氧化活性。结果所有化合物均以较好的收率合成。在这些新化合物中,6c和7c被发现是最有效的,没有神经毒性。所有化合物均表现出清除DPPH自由基的能力,其中化合物7b、7a和6b的清除能力最强。结论这些化合物具有良好的抗惊厥和抗氧化活性,值得临床应用。因此,组的性质对MES模型的抗惊厥活性非常重要。
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