{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,10]],"date-time":"2025-10-10T01:07:00Z","timestamp":1760058420982,"version":"build-2065373602"},"reference-count":34,"publisher":"MDPI AG","issue":"7","license":[{"start":{"date-parts":[[2025,3,31]],"date-time":"2025-03-31T00:00:00Z","timestamp":1743379200000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["21967005","2023GXNSFAA026340","2019KJQD07","2023KTSCX126","2024KCTD012"],"award-info":[{"award-number":["21967005","2023GXNSFAA026340","2019KJQD07","2023KTSCX126","2024KCTD012"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]},{"name":"Natural Science Foundation of Guangxi","award":["21967005","2023GXNSFAA026340","2019KJQD07","2023KTSCX126","2024KCTD012"],"award-info":[{"award-number":["21967005","2023GXNSFAA026340","2019KJQD07","2023KTSCX126","2024KCTD012"]}]},{"name":"Research Start-up Foundation of Guangxi Minzu University","award":["21967005","2023GXNSFAA026340","2019KJQD07","2023KTSCX126","2024KCTD012"],"award-info":[{"award-number":["21967005","2023GXNSFAA026340","2019KJQD07","2023KTSCX126","2024KCTD012"]}]},{"name":"Natural Science Foundation of the Educational Department of Guangdong Province","award":["21967005","2023GXNSFAA026340","2019KJQD07","2023KTSCX126","2024KCTD012"],"award-info":[{"award-number":["21967005","2023GXNSFAA026340","2019KJQD07","2023KTSCX126","2024KCTD012"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>Canthin-6-one alkaloids have consistently attracted the interest of medicinal chemists due to their wide range of promising bioactivities, including antitumor, antifungal, antibacterial, and antiviral properties. However, their low natural abundance in plants has constrained the further exploration of their potential bioactivities. This study reports a comprehensive synthesis of canthin-6-one alkaloids, utilizing key Suzuki coupling and Cu-catalyzed amidation reactions to construct their core scaffold. Derivatives were synthesized with Koenig\u2013Knorr glycosylation for the further modification of synthetic canthin-6-ones. The antimicrobial activities of the synthesized compounds were evaluated against C. albicans,\u00a0C. neoformans, S. aureus and E. coli using the micro-dilution method. In total, 17 compounds were synthesized, including nine canthin-6-ones. Notably, alkaloids 4, 5, 7 and 12-13 were prepared for the first time, along with 8 new derivatives. Their structures were confirmed by NMR and MS analyses. At 50 \u00b5g\/mL, the alkaloids 1-4 and 9 exhibited antimicrobial properties against C. albicans,\u00a0C. neoformans and S. aureus. The antimicrobial activity of alkaloids 2, 4-5 and 12-13 against these four microbial human pathogens is reported here for the first time. Overall, this research not only advances our understanding of canthin-6-one alkaloid synthesis, but also provides a foundation for developing novel compounds with pharmaceutical properties.<\/jats:p>","DOI":"10.3390\/molecules30071546","type":"journal-article","created":{"date-parts":[[2025,3,31]],"date-time":"2025-03-31T02:50:16Z","timestamp":1743389416000},"page":"1546","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["Synthesis and Antimicrobial Activity of Canthin-6-One Alkaloids"],"prefix":"10.3390","volume":"30","author":[{"given":"Xubing","family":"Qi","sequence":"first","affiliation":[{"name":"Key Laboratory of Chemistry and Engineering of Forest Products (State Ethnic Affairs Commission), Guangxi Collaborative Innovation Center for Chemistry and Engineering of Forest Products, School of Chemistry and Chemical Engineering, Guangxi Minzu University, Nanning 530006, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-3869-5288","authenticated-orcid":false,"given":"Yogini","family":"Jaiswal","sequence":"additional","affiliation":[{"name":"Center for Excellence in Post-Harvest Technologies, North Carolina Agricultural and Technical State University, The North Carolina Research Campus, Kannapolis, NC 28081, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Xinrong","family":"Xie","sequence":"additional","affiliation":[{"name":"Key Laboratory of Chemistry and Engineering of Forest Products (State Ethnic Affairs Commission), Guangxi Collaborative Innovation Center for Chemistry and Engineering of Forest Products, School of Chemistry and Chemical Engineering, Guangxi Minzu University, Nanning 530006, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yu","family":"Fan","sequence":"additional","affiliation":[{"name":"Key Laboratory of Chemistry and Engineering of Forest Products (State Ethnic Affairs Commission), Guangxi Collaborative Innovation Center for Chemistry and Engineering of Forest Products, School of Chemistry and Chemical Engineering, Guangxi Minzu University, Nanning 530006, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Rongping","family":"Wu","sequence":"additional","affiliation":[{"name":"Key Laboratory of Chemistry and Engineering of Forest Products (State Ethnic Affairs Commission), Guangxi Collaborative Innovation Center for Chemistry and Engineering of Forest Products, School of Chemistry and Chemical Engineering, Guangxi Minzu University, Nanning 530006, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Shaoyang","family":"Su","sequence":"additional","affiliation":[{"name":"Department of Applied Chemistry Teaching and Research, Guangxi Vocational University of Agriculture, Nanning 530007, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yifu","family":"Guan","sequence":"additional","affiliation":[{"name":"Key Laboratory of Chemistry and Engineering of Forest Products (State Ethnic Affairs Commission), Guangxi Collaborative Innovation Center for Chemistry and Engineering of Forest Products, School of Chemistry and Chemical Engineering, Guangxi Minzu University, Nanning 530006, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0886-5204","authenticated-orcid":false,"given":"Leonard","family":"Williams","sequence":"additional","affiliation":[{"name":"Center for Excellence in Post-Harvest Technologies, North Carolina Agricultural and Technical State University, The North Carolina Research Campus, Kannapolis, NC 28081, USA"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-2566-3519","authenticated-orcid":false,"given":"Xun","family":"Song","sequence":"additional","affiliation":[{"name":"College of Pharmacy, Shenzhen Technology University, Shenzhen 518118, China"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2025,3,31]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"2289","DOI":"10.1080\/14786419.2018.1536708","article-title":"Design, Synthesis and in Vitro Biological Evaluation of Novel 4-Methoxy-5-Hydroxycanthin-6-One Derivatives as Potential Anti-Tumor Agents","volume":"34","author":"Dai","year":"2020","journal-title":"Nat. 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