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Design, synthesis and mechanism against coronavirus of biaryl amide derivatives based on acrylamide covalent warhead
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Zhi-yun WU, Yan-hong LI, Jian-rui LI, Yong-hua LIU, Ying-hong LI, Zong-gen PENG, Dan-qing SONG*
Acta Pharmaceutica Sinica | 2025, 60(9) : 2849 - 2857
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Acta Pharmaceutica Sinica | 2025, 60(9): 2849-2857
• Original Articles •
Design, synthesis and mechanism against coronavirus of biaryl amide derivatives based on acrylamide covalent warhead
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Zhi-yun WU, Yan-hong LI, Jian-rui LI, Yong-hua LIU, Ying-hong LI, Zong-gen PENG, Dan-qing SONG*
Affiliations
  • Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2025-09-12 doi: 10.16438/j.0513-4870.2025-0726
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In this study, a series of novel biaryl amide derivatives featuring an acrylamide covalent warhead were designed and synthesized. The antiviral efficacy of these synthesized compounds against the human β-coronavirus HCoV-OC43 were evaluated using the CCK-8 assay. Among them, compound 6b, containing a 2-fluoroacrylamide covalent warhead, exhibited significant antiviral activity with an EC50 value of 2.52 μmol·L-1 and a selectivity index (SI) of 29, suggesting a reasonable therapeutic window. Molecular docking studies revealed that compound 6bcould inhibit the activities of host transmembrane serine protease 2 (TMPRSS2) and viral 3-chymotrypsin like protease (3CLpro) through covalent bond formation, thereby exerting its antiviral effects. These findings not only expand the structural diversity of this class of compounds but also highlight their potential applications in antiviral therapy. Compound 6brepresents an ideal lead compound for the development of a new class of covalent antiviral drugs against coronaviruses.

biaryl amide derivative  /  β-coronavirus  /  acrylamide covalent warhead  /  transmembrane serine protease 2  /  3-chymotrypsin like protease
吴志云, 李妍红, 李健蕊, 刘永华, 李迎红, 彭宗根, 宋丹青. 基于丙烯酰胺共价弹头的双芳基酰胺衍生物设计合成及抗冠状病毒机制探究. 药学学报, 2025 , 60 (9) : 2849 -2857 . DOI: 10.16438/j.0513-4870.2025-0726
Zhi-yun WU, Yan-hong LI, Jian-rui LI, Yong-hua LIU, Ying-hong LI, Zong-gen PENG, Dan-qing SONG. Design, synthesis and mechanism against coronavirus of biaryl amide derivatives based on acrylamide covalent warhead[J]. Acta Pharmaceutica Sinica, 2025 , 60 (9) : 2849 -2857 . DOI: 10.16438/j.0513-4870.2025-0726
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Year 2025 volume 60 Issue 9
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Article Info
doi: 10.16438/j.0513-4870.2025-0726
  • Receive Date：2025-06-27
  • Online Date：2026-09-20
  • Published：2025-09-12
Article Data
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  • Received：2025-06-27
  • Revised：2025-07-17
Affiliations
    Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
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鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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