Identification of a Small Benzamide Inhibitor of Influenza Virus Using a Cell-Based Screening

Woo Jin Shin, Ky Youb Nam, Nam Doo Kim, Sei Hwan Kim, Kyoung Tai No, Baik Lin Seong

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

Background: The zoonotic transmission of highly pathogenic avian influenza viruses and the global pandemic of H1N1 influenza in 2009 signified the need for a wider coverage of therapeutic options for the control of influenza. Methods: An in-house compound library was screened using a cytopathic effect inhibition assay. Selected hits were then tested in vivo and used as a core skeleton for derivative synthesis. Results: The hit compound (BMD-2601505) was effective [50% effective concentration (EC50) of 60-70 μM] in reducing the death rate of cells infected with human influenza A and B viruses as well as avian influenza A virus. Furthermore, BMD-2601505 reduced the weight loss and increased the survival after lethal infection. The compound was further modified to enhance its antiviral potency. Results show that one derivative with bromobenzene moiety was most effective (EC50 of 22-37 μM) against the influenza viruses tested. Conclusion: We identified a small benzamide compound exhibiting antiviral activity against influenza viruses. The results warrant further evaluation of antiviral activities against drug-resistant influenza isolates.

Original languageEnglish
Pages (from-to)159-166
Number of pages8
JournalChemotherapy
Volume61
Issue number3
DOIs
Publication statusPublished - 2016 Apr 1

Fingerprint

Orthomyxoviridae
Human Influenza
Antiviral Agents
Influenza in Birds
Influenza A virus
Influenza B virus
Zoonoses
Pandemics
Skeleton
Libraries
Weight Loss
Mortality
benzamide
Infection
Pharmaceutical Preparations
Therapeutics

All Science Journal Classification (ASJC) codes

  • Oncology
  • Pharmacology
  • Drug Discovery
  • Pharmacology (medical)
  • Infectious Diseases

Cite this

Shin, Woo Jin ; Nam, Ky Youb ; Kim, Nam Doo ; Kim, Sei Hwan ; No, Kyoung Tai ; Seong, Baik Lin. / Identification of a Small Benzamide Inhibitor of Influenza Virus Using a Cell-Based Screening. In: Chemotherapy. 2016 ; Vol. 61, No. 3. pp. 159-166.
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Identification of a Small Benzamide Inhibitor of Influenza Virus Using a Cell-Based Screening. / Shin, Woo Jin; Nam, Ky Youb; Kim, Nam Doo; Kim, Sei Hwan; No, Kyoung Tai; Seong, Baik Lin.

In: Chemotherapy, Vol. 61, No. 3, 01.04.2016, p. 159-166.

Research output: Contribution to journalArticle

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