{"title":"Effective synthesis and anti-mycobacteriuml activity of isoxazole-substituted pyrrolopyrimidine and isoxazole-substituted indole derivatives","authors":"Yafei Xue, Yongchang Bi, Jingjun Wang, Guangyuan Zhu, Mingyue Chen, Xingyu Bian, Yumin Zhang, Qiang Gu","doi":"10.1007/s13738-025-03196-x","DOIUrl":null,"url":null,"abstract":"<div><p>Isoxazole-containing compounds showed an array of biological activities relevant to pulmonary tuberculosis. A series of pyrrolopyrimidine and indole derivatives containing isoxazole rings were constructed and synthesized by employing substituted isoxazole, pyrrolopyrimidine and indole derivatives as raw materials under the optimal reaction condition. On the basis of confirming the structure of the synthesized compounds, their antibacterial activity against <i>Mycobacteria smegmatis</i> in vitro was evaluated using rifampin as a positive control. Two compounds showed excellent anti-mycobacterium activity, and their minimum inhibitory concentrations were respectively 10.67 ± 3.77 μg/mL and 8.00 μg/mL, which suggested that they can be regarded as candidates for development of anti-tuberculosis drugs.</p><h3>Graphical abstract</h3>\n<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":676,"journal":{"name":"Journal of the Iranian Chemical Society","volume":"22 5","pages":"969 - 977"},"PeriodicalIF":2.2000,"publicationDate":"2025-04-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of the Iranian Chemical Society","FirstCategoryId":"92","ListUrlMain":"https://link.springer.com/article/10.1007/s13738-025-03196-x","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
引用次数: 0
Abstract
Isoxazole-containing compounds showed an array of biological activities relevant to pulmonary tuberculosis. A series of pyrrolopyrimidine and indole derivatives containing isoxazole rings were constructed and synthesized by employing substituted isoxazole, pyrrolopyrimidine and indole derivatives as raw materials under the optimal reaction condition. On the basis of confirming the structure of the synthesized compounds, their antibacterial activity against Mycobacteria smegmatis in vitro was evaluated using rifampin as a positive control. Two compounds showed excellent anti-mycobacterium activity, and their minimum inhibitory concentrations were respectively 10.67 ± 3.77 μg/mL and 8.00 μg/mL, which suggested that they can be regarded as candidates for development of anti-tuberculosis drugs.
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JICS is an international journal covering general fields of chemistry. JICS welcomes high quality original papers in English dealing with experimental, theoretical and applied research related to all branches of chemistry. These include the fields of analytical, inorganic, organic and physical chemistry as well as the chemical biology area. Review articles discussing specific areas of chemistry of current chemical or biological importance are also published. JICS ensures visibility of your research results to a worldwide audience in science. You are kindly invited to submit your manuscript to the Editor-in-Chief or Regional Editor. All contributions in the form of original papers or short communications will be peer reviewed and published free of charge after acceptance.
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