Scalable Synthesis, In Vitro cccDNA Reduction, and In Vivo Antihepatitis B Virus Activity of a Phosphonomethoxydeoxythreosyl Adenine Prodrug

Author:

Luo Min1,Wu Shuo2,Kalkeri Raj3,Ptak Roger G.3,Zhou Tianlun4,Van Mellaert Lieve5,Wang Chuanmin6,Dumbre Shrinivas G.1,Block Timothy4,Groaz Elisabetta1,De Jonghe Steven7ORCID,Li Yuhuan2,Herdewijn Piet1ORCID

Affiliation:

1. Medicinal Chemistry, KU Leuven, Rega Institute for Medical Research, Herestraat 49-box 1041, 3000 Leuven, Belgium

2. CAMS Key Laboratory of Antiviral Drug Research, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, No. 1, Tiantan Xili, 100050 Beijing, China

3. Department of Infectious Disease Research, Southern Research Institute, 431 Aviation Way, Frederick, Maryland 21701, United States

4. Baruch S. Blumberg Institute, Doylestown, Pennsylvania 18902, United States

5. Department of Microbiology, Immunology and Transplantation, Laboratory of Molecular Bacteriology, KU Leuven, Rega Institute for Medical Research, Herestraat 49-box 1037, 3000 Leuven, Belgium

6. Department of Infectious Diseases, Taihe Hospital, Hubei University of Medicine, Shiyan, Hubei 442000, China

7. Department of Microbiology, Immunology and Transplantation, Laboratory of Virology and Chemotherapy, KU Leuven, Rega Institute for Medical Research, Herestraat 49-box 1043, 3000 Leuven, Belgium

Funder

KU Leuven

National Institute of Allergy and Infectious Diseases

The Drug Innovation Major Project

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Reference35 articles.

1. World Health Organization About Viral Hepatitis. 2019. WHO, https://www.who.int/hepatitis/about/en/ (accessed Nov 28, 2020).web

2. Hepatitis B virus infection

3. HBV replication inhibitors

4. Replication of the genome of a hepatitis B-like virus by reverse transcription of an RNA intermediate

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