{"title":"含吲哚-3-甲基（苯基）氨基侧链的三唑醇对耐氟康唑白色念珠菌的合成及生物学评价","authors":"Zefei Fan, Lijiao Yang, Jidong Wang, Yafei Hou, Fei Zou, Tianyu Zhang, Yongyan Fu, Yue Zhang, Ruirui Wang, Shichong Yu, Guanghui Ni","doi":"10.1007/s00044-025-03469-3","DOIUrl":null,"url":null,"abstract":"<div><p>A novel series of triazole alcohols containing an indole-3-methyl(phenyl)a- mino side chain have been synthesized as derivatives of fluconazole. The title compounds were synthesized via the ring-open reaction of epoxide with various N-aryl indole-3-methylamine. Compound <b>C04</b> exhibited significant inhibitory activity against fluconazole-resistant <i>Candida albicans</i> (ATCC-14053) with an MIC<sub>50</sub> of 2.31 μM. Notably, compound <b>C08</b> displayed potent inhibition against seven fungal pathogens including two clinically isolated fluconazole-resistant strains. The time-kill assays demonstrated that compounds C04 and C08 exhibited significant growth inhibitory effects against <i>Candida albicans</i> ATCC 14053. Further studies confirmed their potent inhibitory activity against <i>C. albicans</i> biofilm development. Cytotoxicity evaluation demonstrated that both compounds exhibited favorable safety profiles. These results indicate that <b>C04</b> and <b>C08</b> are promising antifungal drug candidates, providing novel therapeutic strategies to combat clinically resistant fungal infections.</p><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"34 10","pages":"2179 - 2194"},"PeriodicalIF":3.1000,"publicationDate":"2025-09-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s00044-025-03469-3.pdf","citationCount":"0","resultStr":"{\"title\":\"Synthesis and biological evaluation of triazole alcohols containing an indole-3-methyl(phenyl)amino side chain against fluconazole-resistant Candida albicans\",\"authors\":\"Zefei Fan, Lijiao Yang, Jidong Wang, Yafei Hou, Fei Zou, Tianyu Zhang, Yongyan Fu, Yue Zhang, Ruirui Wang, Shichong Yu, Guanghui Ni\",\"doi\":\"10.1007/s00044-025-03469-3\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>A novel series of triazole alcohols containing an indole-3-methyl(phenyl)a- mino side chain have been synthesized as derivatives of fluconazole. The title compounds were synthesized via the ring-open reaction of epoxide with various N-aryl indole-3-methylamine. Compound <b>C04</b> exhibited significant inhibitory activity against fluconazole-resistant <i>Candida albicans</i> (ATCC-14053) with an MIC<sub>50</sub> of 2.31 μM. Notably, compound <b>C08</b> displayed potent inhibition against seven fungal pathogens including two clinically isolated fluconazole-resistant strains. The time-kill assays demonstrated that compounds C04 and C08 exhibited significant growth inhibitory effects against <i>Candida albicans</i> ATCC 14053. Further studies confirmed their potent inhibitory activity against <i>C. albicans</i> biofilm development. Cytotoxicity evaluation demonstrated that both compounds exhibited favorable safety profiles. These results indicate that <b>C04</b> and <b>C08</b> are promising antifungal drug candidates, providing novel therapeutic strategies to combat clinically resistant fungal infections.</p><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>\",\"PeriodicalId\":699,\"journal\":{\"name\":\"Medicinal Chemistry Research\",\"volume\":\"34 10\",\"pages\":\"2179 - 2194\"},\"PeriodicalIF\":3.1000,\"publicationDate\":\"2025-09-20\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://link.springer.com/content/pdf/10.1007/s00044-025-03469-3.pdf\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Medicinal Chemistry Research\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://link.springer.com/article/10.1007/s00044-025-03469-3\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Medicinal Chemistry Research","FirstCategoryId":"3","ListUrlMain":"https://link.springer.com/article/10.1007/s00044-025-03469-3","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
Synthesis and biological evaluation of triazole alcohols containing an indole-3-methyl(phenyl)amino side chain against fluconazole-resistant Candida albicans
A novel series of triazole alcohols containing an indole-3-methyl(phenyl)a- mino side chain have been synthesized as derivatives of fluconazole. The title compounds were synthesized via the ring-open reaction of epoxide with various N-aryl indole-3-methylamine. Compound C04 exhibited significant inhibitory activity against fluconazole-resistant Candida albicans (ATCC-14053) with an MIC50 of 2.31 μM. Notably, compound C08 displayed potent inhibition against seven fungal pathogens including two clinically isolated fluconazole-resistant strains. The time-kill assays demonstrated that compounds C04 and C08 exhibited significant growth inhibitory effects against Candida albicans ATCC 14053. Further studies confirmed their potent inhibitory activity against C. albicans biofilm development. Cytotoxicity evaluation demonstrated that both compounds exhibited favorable safety profiles. These results indicate that C04 and C08 are promising antifungal drug candidates, providing novel therapeutic strategies to combat clinically resistant fungal infections.
期刊介绍：
Medicinal Chemistry Research (MCRE) publishes papers on a wide range of topics, favoring research with significant, new, and up-to-date information. Although the journal has a demanding peer review process, MCRE still boasts rapid publication, due in part, to the length of the submissions. The journal publishes significant research on various topics, many of which emphasize the structure-activity relationships of molecular biology.
求助内容：
应助结果提醒方式：
京公网安备 11010802042870号
