Phenolic diterpenoid derivatives as anti-influenza a virus agents

  • ACS Med Chem Lett. 2015 Jan 29;6(3):355-8. doi: 10.1021/ml500533x.
Zhao Dang  1 ,  Katherine Jung  1 ,  Lei Zhu  1 ,  Hua Xie  2 ,  Kuo-Hsiung Lee  3 ,  Chin-Ho Chen  1 ,  Li Huang  1
Affiliations
  • 1. Surgical Science, Department of Surgery, Duke University Medical Center , Durham, North Carolina 27710, United States.
  • 2. School of Dentistry, Meharry Medical College , Nashville, Tennessee 37208, United States.
  • 3. Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina , Chapel Hill, North Carolina 27599, United States ; Chinese Medicine Research and Development Center, China Medical University and Hospital , Taichung, Taiwan.
PMID: 25815159 DOI: 10.1021/ml500533x
Abstract

A series of diterpenoid derivatives based on podocarpic acid were synthesized and evaluated as anti-influenza A virus agents. Several of the novel podocarpic acid derivatives exhibited nanomolar activities against an H1N1 influenza A virus (A/Puerto Rico/8/34) that was resistant to two anti-influenza drugs, oseltamivir and amantadine. This class of compounds inhibits the Influenza Virus by targeting the viral hemagglutinin-mediated membrane fusion. These results indicated that podocarpic acid derivatives may serve as potential drug candidates to fight drug-resistant influenza A virus infections.

Keywords
Influenza A; hemagglutinin; influenza inhibitor; podocarpic acid; totarol.