松香、枞酸和胡椒酸二肽 Ugi-4CR 衍生物及其抗甲型流感病毒和 SARS-CoV-2 的活性。
Abietic, maleopimaric and quinopimaric dipeptide Ugi-4CR derivatives and their potency against influenza A and SARS-CoV-2.
机构信息
Ufa Institute of Chemistry of the Ufa Federal Research Centre of the Russian Academy of Sciences, Ufa, Russian Federation.
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, China.
出版信息
Nat Prod Res. 2023 Jun;37(12):1954-1960. doi: 10.1080/14786419.2022.2112040. Epub 2022 Aug 17.
A set of 12 abietane diterpene derivatives have been synthesised by the Ugi-four component reaction (Ugi-4CR) and tested for cytotoxicity and activity against influenza virus A/Puerto Rico/8/34 (H1N1) and SARS-CoV-2 pseudovirus. Five dipeptide derivatives demonstrated a selectivity index (SI) higher than 10 and IC values from 2 to 32 μM against influenza virus. Compound was found to be a lead with SI of 200, and time-of-addition experiments showed the viral entry into the cell and the binding of the virus to the receptor as a possible target. Compound was the only one showed weak anti-SARS-CoV-2 activity with EC value of 80.96 µM. Taken together, our data suggest the potency of diterpene acids-Ugi products as new effective anti-influenza compounds.
通过 Ugi-4CR 反应合成了 12 个松香烷二萜衍生物，并对其进行了细胞毒性测试以及对甲型流感病毒 A/Puerto Rico/8/34（H1N1）和 SARS-CoV-2 假病毒的活性测试。五种二肽衍生物对流感病毒表现出高于 10 的选择性指数（SI）和 2 至 32μM 的 IC 值。化合物 被认为是具有 200 的 SI 的先导化合物，加药时间实验表明病毒进入细胞以及病毒与受体的结合可能是其作用靶点。化合物 是唯一显示出对 SARS-CoV-2 具有弱抑制活性的化合物，EC 值为 80.96μM。综上所述，我们的数据表明二萜酸-Ugi 产物具有作为新型有效抗流感化合物的潜力。
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