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Analgesic Activity and Acute Toxicity of Dihydrotetrazolo[1,5-a]Pyrimidine Derivatives
Pharmaceutical Chemistry Journal ( IF 0.8 ) Pub Date : 2021-06-14 , DOI: 10.1007/s11094-021-02403-2
V. L. Gein , A. N. Prudnikova , A. A. Kurbatova , I. P. Rudakova

Aseries of dihydrotetrazolo[1,5-a]pyrimidine derivatives were synthesized via a three-component reaction of benzoylacetone with aromatic aldehydes and 5-aminotetrazole monohydrate. The obtained compounds were tested for analgesic activity using the acetic acid-induced writhing test. Their acute toxicities were determined. (7-Aryl-5-methyl-4,7-dihydrotetrazolo[1,5-a]pyrimidin-6-yl)(phenyl)methanones were found to exhibit analgesic activity comparable to that of the reference drug metamizole sodium and were low-toxicity compounds. The obtained results were indicative of good prospects for further investigation of analgesic properties in this series of compounds.



中文翻译:

二氢四唑并[1,5-a]嘧啶衍生物的镇痛活性和急性毒性

通过苯甲酰丙酮与芳香醛和 5-氨基四唑一水合物的三组分反应合成了一系列二氢四唑并[1,5- a ]嘧啶衍生物。使用乙酸诱导的扭体试验测试所得化合物的镇痛活性。确定了它们的急性毒性。(7-Aryl-5-methyl-4,7-dihydrotetrazolo[1,5- a ]pyrimidin-6-yl)(phenyl)methanones 被发现表现出与参考药物安乃近钠相当的镇痛活性,并且低毒性化合物。获得的结果表明进一步研究该系列化合物的镇痛特性具有良好的前景。

更新日期:2021-06-14
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