Harnessing Natural Products by a Pharmacophore‐Oriented Semisynthesis Approach for the Discovery of Potential Anti‐SARS‐CoV‐2 Agents
| العنوان: | Harnessing Natural Products by a Pharmacophore‐Oriented Semisynthesis Approach for the Discovery of Potential Anti‐SARS‐CoV‐2 Agents |
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| المؤلفون: | Yuan‐Fei Zhou, Bing‐Chao Yan, Qian Yang, Xin‐Yan Long, Dan‐Qi Zhang, Rong‐Hua Luo, Han‐Yu Wang, Han‐Dong Sun, Xiao‐Song Xue, Yong‐Tang Zheng, Pema‐Tenzin Puno |
| المصدر: | Angewandte Chemie. 134 |
| بيانات النشر: | Wiley, 2022. |
| سنة النشر: | 2022 |
| مصطلحات موضوعية: | Biological Products, SARS-CoV-2, Humans, General Chemistry, General Medicine, Antiviral Agents, Catalysis, COVID-19 Drug Treatment |
| الوصف: | Natural products possessing unique scaffolds may have antiviral activity but their complex structures hinder facile synthesis. A pharmacophore-oriented semisynthesis approach was applied to (-)-maoelactone A (1) and oridonin (2) for the discovery of anti-SARS-CoV-2 agents. The Wolff rearrangement/lactonization cascade (WRLC) reaction was developed to construct the unprecedented maoelactone-type scaffold during semisynthesis of 1. Further mechanistic study suggested a concerted mechanism for Wolff rearrangement and a water-assisted stepwise process for lactonization. The WRLC reaction then enabled the creation of a novel family by assembly of the maoelactone-type scaffold and the pharmacophore of 2, whereby one derivative inhibited SARS-CoV-2 replication in HPA EpiC cells with a low EC |
| تدمد: | 1521-3757 0044-8249 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bfda10ac1021e2323995a536b5be40b5 https://doi.org/10.1002/ange.202201684 |
| حقوق: | CLOSED |
| رقم الأكسشن: | edsair.doi.dedup.....bfda10ac1021e2323995a536b5be40b5 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 15213757 00448249 |
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