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Discovery and SAR Research for Antivirus Activity of Novel Butenolide on Influenza A Virus H1N1 In Vitro and In Vivo.

ABSTRACT: Influenza viruses (IV) cause substantial morbidity and mortality through routine seasonal spread and epidemics. A novel series of butenolides were discovered to be able to inhibit influenza H1N1 activity in vitro, and the SAR for anti-influenza activity was investigated. By optimization of the hit compound, compound 37 was obtained with an EC₅₀ of 6.7 ?M against influenza A virus H1N1 as an inhibitor of NA and with low cytotoxicity on MDCK cells. Also, it can inhibit the expression of the influenza A virus gene in the lung of SPF KM mice to show antivirus activity in vivo. These results suggested that compound 37 could inhibit the influenza A virus H1N1 via targeting NA.

SUBMITTER: Wang Z

PROVIDER: S-EPMC6705239 | biostudies-literature | 2019 Aug

REPOSITORIES: biostudies-literature

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Discovery and SAR Research for Antivirus Activity of Novel Butenolide on Influenza A Virus H1N1 In Vitro and In Vivo.

Wang Zhenya Z Hu Xiaoning X Li Yuanyuan Y Mou Xiaodong X Wang Congcong C Chen Xinli X Tan Yayun Y Wu Chunli C Liu Hongmin H Xu Haiwei H

ACS omega 20190802 8

Influenza viruses (IV) cause substantial morbidity and mortality through routine seasonal spread and epidemics. A novel series of butenolides were discovered to be able to inhibit influenza H1N1 activity in vitro, and the SAR for anti-influenza activity was investigated. By optimization of the hit compound, compound <b>37</b> was obtained with an EC<sub>50</sub> of 6.7 μM against influenza A virus H1N1 as an inhibitor of NA and with low cytotoxicity on MDCK cells. Also, it can inhibit the expres ...[more]

PMID: 31460454

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