Synthesis of novel entecavir analogues having 4′-cyano-6′′-fluoromethylenecyclopentene skeletons as an aglycone moiety as highly potent and long-acting anti-hepatitis B virus agent

Author:

Kumamoto Hiroki1,Higashi-Kuwata Nobuyo2ORCID,Hayashi Sanae3,Das Debananda4,Bulut Haydar4,Tokuda Ryoh5,Imoto Shuhei5,Onitsuka Kengo2,Honda Yuka6,Odanaka Yuki6,Shimbara-Matsubayashi Satoko6,Haraguchi Kazuhiro1,Tanaka Yasuhito3,Mitsuya Hiroaki247

Affiliation:

1. Department of Pharmaceutical Sciences, Nihon Pharmaceutical University, Saitama, Japan

2. Department of Refractory Viral Infection, National Center for Global Health & Medicine Research Institute, Tokyo, Japan

3. Department of Gastroenterology and Hepatology, Faculty of Life Sciences, Kumamoto University, Kumamoto, Japan

4. Experimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, MD, USA

5. Faculty of Pharmaceutical Sciences, Sojo University, Kumamoto, Japan

6. School of Pharmacy, Showa University, Tokyo, Japan

7. Department of Clinical Sciences, Kumamoto University Hospital, Kumamoto, Japan

Abstract

Encouraged by our recent findings that 4′-cyano-deoxyguanosine (2), entecavir analogues 4 and 5 are highly potent anti-hepatitis B virus (HBV) agents, we designed and synthesized 6 having a hybridized structure of 4 and 5.

Funder

Japan Agency for Medical Research and Development

Japan Society for the Promotion of Science

National Cancer Institute

National Institutes of Health

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemical Engineering,General Chemistry

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