{"title":"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","authors":"Nedime Çalışkan , Gülay Akyüz , Emre Menteşe","doi":"10.1080/10426507.2024.2333471","DOIUrl":null,"url":null,"abstract":"<div><p>In this study, a new series of 3<em>H-</em>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,<sup>1</sup>H, and <sup>13</sup>C NMR spectral data. The antiurease activities of all new compounds were tested according to the method by Weatherburn. The inhibition results with the 3<em>H-</em>quinazoline-4-thione ring compounds were compared with those of some previously synthesized 3<em>H-</em>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(3<em>H</em>)-thione (<strong>2i</strong>) has the best inhibition results with IC<sub>50</sub> = 1.6 ± 0.049 μg/mL.</p></div>","PeriodicalId":20056,"journal":{"name":"Phosphorus, Sulfur, and Silicon and the Related Elements","volume":"199 4","pages":"Pages 293-298"},"PeriodicalIF":1.4000,"publicationDate":"2024-04-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"A facile ultrasonic synthesis approach to 3-H-quinazolinethione derivatives and their urease inhibition studies\",\"authors\":\"Nedime Çalışkan , Gülay Akyüz , Emre Menteşe\",\"doi\":\"10.1080/10426507.2024.2333471\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>In this study, a new series of 3<em>H-</em>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,<sup>1</sup>H, and <sup>13</sup>C NMR spectral data. The antiurease activities of all new compounds were tested according to the method by Weatherburn. The inhibition results with the 3<em>H-</em>quinazoline-4-thione ring compounds were compared with those of some previously synthesized 3<em>H-</em>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(3<em>H</em>)-thione (<strong>2i</strong>) has the best inhibition results with IC<sub>50</sub> = 1.6 ± 0.049 μg/mL.</p></div>\",\"PeriodicalId\":20056,\"journal\":{\"name\":\"Phosphorus, Sulfur, and Silicon and the Related Elements\",\"volume\":\"199 4\",\"pages\":\"Pages 293-298\"},\"PeriodicalIF\":1.4000,\"publicationDate\":\"2024-04-02\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Phosphorus, Sulfur, and Silicon and the Related Elements\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://www.sciencedirect.com/org/science/article/pii/S1042650724000121\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"CHEMISTRY, INORGANIC & NUCLEAR\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Phosphorus, Sulfur, and Silicon and the Related Elements","FirstCategoryId":"92","ListUrlMain":"https://www.sciencedirect.com/org/science/article/pii/S1042650724000121","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"CHEMISTRY, INORGANIC & NUCLEAR","Score":null,"Total":0}
A facile ultrasonic synthesis approach to 3-H-quinazolinethione derivatives and their urease inhibition studies
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.
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.