A facile ultrasonic synthesis approach to 3-H-quinazolinethione derivatives and their urease inhibition studies

IF 16.4 1区 化学 Q1 CHEMISTRY, MULTIDISCIPLINARY Accounts of Chemical Research Pub Date : 2024-04-02 DOI:10.1080/10426507.2024.2333471
Nedime Çalışkan , Gülay Akyüz , Emre Menteşe
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Abstract

In this study, a new series of 3H-quinazoline-4-thione derivatives were synthesized under ultrasonic irradiation conditions with high yield in a short time. The new compounds were characterized by FT-IR,1H, and 13C NMR spectral data. The antiurease activities of all new compounds were tested according to the method by Weatherburn. The inhibition results with the 3H-quinazoline-4-thione ring compounds were compared with those of some previously synthesized 3H-quinazolin-4-ones. More effective results were found for most quinazolinethione compounds. All new synthesized compounds have effective urease inhibition activity. Especially, the compound 2-(4-nitrobenzyl)quinazoline-4(3H)-thione (2i) has the best inhibition results with IC50 = 1.6 ± 0.049 μg/mL.

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3- H -喹唑啉硫酮衍生物的简便超声合成方法及其脲酶抑制研究
本研究在超声波辐照条件下合成了一系列新的 3H-喹唑啉-4-硫酮衍生物,并在短时间内获得了高产率。通过傅立叶变换红外光谱、1H 和 13C NMR 光谱数据对新化合物进行了表征。根据 Weatherburn 的方法对所有新化合物的抗尿酸酶活性进行了测试。将 3H-喹唑啉-4-硫酮环化合物的抑制结果与之前合成的一些 3H-喹唑啉-4-酮化合物的抑制结果进行了比较。结果发现,大多数喹唑啉硫酮化合物的抑制效果更好。所有新合成的化合物都具有有效的脲酶抑制活性。尤其是化合物 2-(4-硝基苄基)喹唑啉-4(3H)-硫酮(2i)的抑制效果最好,IC50 = 1.6 ± 0.049 μg/mL。
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来源期刊
Accounts of Chemical Research
Accounts of Chemical Research 化学-化学综合
CiteScore
31.40
自引率
1.10%
发文量
312
审稿时长
2 months
期刊介绍: Accounts of Chemical Research presents short, concise and critical articles offering easy-to-read overviews of basic research and applications in all areas of chemistry and biochemistry. These short reviews focus on research from the author’s own laboratory and are designed to teach the reader about a research project. In addition, Accounts of Chemical Research publishes commentaries that give an informed opinion on a current research problem. Special Issues online are devoted to a single topic of unusual activity and significance. Accounts of Chemical Research replaces the traditional article abstract with an article "Conspectus." These entries synopsize the research affording the reader a closer look at the content and significance of an article. Through this provision of a more detailed description of the article contents, the Conspectus enhances the article's discoverability by search engines and the exposure for the research.
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