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The convergent route featured a novel one-step C\u2013H functionalization of aniline to form the benzothiazole ring, a double Suzuki\u2013Miyaura coupling to construct the thiazole-fused p-terphenyl core, and late-stage dehydrogenative couplings to afford nocarterphenyls divergently. Biological evaluation indicated that these natural products and their derivatives represent a new class of potent \u03b1-glucosidase inhibitors. Among all tested compounds, nocarterphenyl derivative 5 exhibited the strongest inhibitory effect, with an IC50 value of 9.82 \u00b1 0.31 \u03bcM, which was markedly greater than that of the positive control acarbose (570 \u00b1 4.40 \u03bcM). Enzyme kinetic assays demonstrated compound 5 to be a reversible, mixed-type \u03b1-glucosidase inhibitor. Circular dichroism (CD) spectroscopy further revealed that the binding of compound 5 induced pronounced conformational alterations and obvious changes in the microenvironment surrounding the secondary structure of \u03b1-glucosidase.<\/jats:p>","DOI":"10.1021\/acs.joc.6c01869","type":"journal-article","created":{"date-parts":[[2026,10,5]],"date-time":"2026-10-05T20:01:12Z","timestamp":1791230472000},"page":"14431-14443","source":"Crossref","is-referenced-by-count":0,"title":["Total Synthesis of Nocarterphenyls A-B and 2-Dehydroxymethylnocarterphenyl A, Formal Synthesis of Nocarterphenyl D, and Biological Evaluation of Nocarterphenyls as \u03b1-Glucosidase Inhibitors"],"prefix":"10.1021","volume":"91","author":[{"given":"Huan","family":"Zhou","sequence":"first","affiliation":[{"name":"Guangzhou Huali College , , ,","place":["Jiangmen, China, 529100"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0009-0001-6312-7610","authenticated-orcid":true,"given":"Xiaotong","family":"Liu","sequence":"additional","affiliation":[{"name":"Wuyi University , , , ,","place":["Jiangmen, Guangdong, China, 529020"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yuanyi","family":"Cen","sequence":"additional","affiliation":[{"name":"Wuyi University , , , ,","place":["Jiangmen, Guangdong, China, 529020"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Panyang","family":"Li","sequence":"additional","affiliation":[{"name":"Wuyi University , , , ,","place":["Jiangmen, Guangdong, China, 529020"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xuetao","family":"Xu","sequence":"additional","affiliation":[{"name":"Wuyi University , , , ,","place":["Jiangmen, Guangdong, China, 529020"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3804-9507","authenticated-orcid":true,"given":"Jia-Lei","family":"Yan","sequence":"additional","affiliation":[{"name":"Wuyi University , , , ,","place":["Jiangmen, Guangdong, China, 529020"]},{"name":"Jinan University , , ,","place":["Guangzhou, China, 510632"]}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"316","published-online":{"date-parts":[[2026,10,5]]},"reference":[{"key":"2026103005070046400_cit1a","doi-asserted-by":"publisher","first-page":"1","DOI":"10.1080\/10286020.2017.1381089","article-title":"Structural and biological diversity of natural p-terphenyls","volume":"20","author":"Li","year":"2018","journal-title":"J. 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