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

IF 1.4 4区 化学 Q4 CHEMISTRY, INORGANIC & NUCLEAR
Nedime Çalışkan , Gülay Akyüz , Emre Menteşe
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引用次数: 0

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.

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
CiteScore
2.60
自引率
7.70%
发文量
103
审稿时长
2.1 months
期刊介绍: Phosphorus, Sulfur, and Silicon and the Related Elements is a monthly publication intended to disseminate current trends and novel methods to those working in the broad and interdisciplinary field of heteroatom chemistry.
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