3-Hydroxypyrimidine-2,4-Diones as Novel Hepatitis B Virus Antivirals Targeting the Viral Ribonuclease H
| Autor: | Maxwell D. Leslie, Michael A. Parniak, Kelsey N. Boschert, Maritza Puray-Chavez, Karen A. Kirby, Zhengqiang Wang, Andrew D. Huber, Jing Tang, Kamalendra Singh, Hiroaki Mitsuya, Maria Boftsi, Megan A. Sheridan, Stefan G. Sarafianos, Eleftherios Michailidis, Jennifer J. Wolf |
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| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Hepatitis B virus Hepatitis B virus DNA polymerase Ribonuclease H Virus Replication medicine.disease_cause Antiviral Agents Hepatitis B virus PRE beta 03 medical and health sciences medicine Humans Pharmacology (medical) RNase H Pharmacology biology Chemistry virus diseases Hbv replication Virology digestive system diseases NS2-3 protease 030104 developmental biology Infectious Diseases Viral replication biology.protein |
| Zdroj: | Antimicrobial Agents and Chemotherapy. 61 |
| ISSN: | 1098-6596 0066-4804 |
| DOI: | 10.1128/aac.00245-17 |
| Popis: | Hepatitis B virus (HBV) RNase H (RNH) is an appealing therapeutic target due to its essential role in viral replication. RNH inhibitors (RNHIs) could help to more effectively control HBV infections. Here, we report 3-hydroxypyrimidine-2,4-diones as novel HBV RNHIs with antiviral activity. We synthesized and tested 52 analogs and found 4 that inhibit HBV RNH activity in infected cells. Importantly, 2 of these compounds inhibited HBV replication in the low micromolar range. |
| Databáze: | OpenAIRE |
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