Green Synthesis and Biological Evaluation of Some 1,2,4-Triazol-3-ones

IF 0.8 4区 化学 Q4 CHEMISTRY, ORGANIC
F. Yilmaz
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引用次数: 0

Abstract

A series of 1,2,4-triazol-3-one derivatives were synthesized by using conventional heating and microwave irradiation techniques. Microwave syntheses of the target compounds were carried out by using both a domestic microwave oven and a monomode microwave reactor. The results showed that the use of microwave technique is advantageous in terms of time, low solvent loading, yield, and efficiency. The synthesized compounds were tested for their antioxidant and antiurease activities. The antioxidant activity was evaluated by using ABTS [2,2′-azinobis(3-ethylbenzothiazoline-6-sulphonic acid) diammonium salt] radical scavenging and cupric ion reducing antioxidant capacity (CUPRAC) methods. Most of the compounds showed good antioxidant activity, especially compound 8d showed an SC50 value of 71.062±9.31 μM in comparison to Trolox used as standard (SC50 = 210.04±16.22 μM). According to the urease inhibitory activity results, most of the compounds showed better activity than thiourea (IC50 = 0.5027±0.0293 μM); in particular, compound 8a exhibited an IC50 value of 0.3070±0.0394 μM.

Abstract Image

一些 1,2,4-三唑-3-酮的绿色合成与生物学评价
摘要 采用常规加热和微波辐照技术合成了一系列 1,2,4-三唑-3-酮衍生物。使用家用微波炉和单模微波反应器对目标化合物进行了微波合成。结果表明,使用微波技术在时间、低溶剂负荷、产率和效率方面具有优势。对合成的化合物进行了抗氧化和抗尿毒症活性测试。抗氧化活性采用 ABTS [2,2′-azinobis(3-ethylbenzothiazoline-6-sulphonic acid) diammonium salt] 自由基清除法和铜离子还原抗氧化能力(CUPRAC)法进行评估。大多数化合物表现出良好的抗氧化活性,尤其是化合物 8d 的 SC50 值为 71.062±9.31 μM,而标准品为三氯氧磷(SC50 = 210.04±16.22 μM)。根据脲酶抑制活性结果,大多数化合物显示出比硫脲更好的活性(IC50 = 0.5027±0.0293 μM),特别是化合物 8a 的 IC50 值为 0.3070±0.0394 μM。
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来源期刊
CiteScore
1.40
自引率
25.00%
发文量
139
审稿时长
3-6 weeks
期刊介绍: Russian Journal of Organic Chemistry is an international peer reviewed journal that covers all aspects of modern organic chemistry including organic synthesis, theoretical organic chemistry, structure and mechanism, and the application of organometallic compounds in organic synthesis.
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