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  1. Article ; Online: Synthesis of 4'-Substituted Carbocyclic Uracil Derivatives and Their Monophosphate Prodrugs as Potential Antiviral Agents.

    Biteau, Nicolas G / Amichai, Sarah A / Azadi, Niloufar / De, Ramyani / Downs-Bowen, Jessica / Lecher, Julia C / MacBrayer, Tamara / Schinazi, Raymond F / Amblard, Franck

    Viruses

    2023  Volume 15, Issue 2

    Abstract: Over the past decades, both 4'-modified nucleoside and carbocyclic nucleoside analogs have been under the spotlight as several compounds from either family showed anti-HIV, HCV, RSV or SARS-CoV-2 activity. Herein, we designed compounds combining these ... ...

    Abstract Over the past decades, both 4'-modified nucleoside and carbocyclic nucleoside analogs have been under the spotlight as several compounds from either family showed anti-HIV, HCV, RSV or SARS-CoV-2 activity. Herein, we designed compounds combining these two features and report the synthesis of a series of novel 4'-substituted carbocyclic uracil derivatives along with their corresponding monophosphate prodrugs. These compounds were successfully prepared in 19 to 22 steps from the commercially available (-)-Vince lactam and were evaluated against a panel of RNA viruses including SARS-CoV-2, influenza A/B viruses and norovirus.
    MeSH term(s) Humans ; Antiviral Agents/pharmacology ; COVID-19 ; Hepatitis C Antibodies ; Influenza A virus ; Influenza B virus ; Nucleosides ; Prodrugs/pharmacology ; SARS-CoV-2 ; Uracil
    Chemical Substances Antiviral Agents ; Hepatitis C Antibodies ; Nucleosides ; Prodrugs ; Uracil (56HH86ZVCT)
    Language English
    Publishing date 2023-02-16
    Publishing country Switzerland
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Research Support, N.I.H., Extramural
    ZDB-ID 2516098-9
    ISSN 1999-4915 ; 1999-4915
    ISSN (online) 1999-4915
    ISSN 1999-4915
    DOI 10.3390/v15020544
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Synthesis and evaluation of highly potent HBV capsid assembly modulators (CAMs).

    Amblard, Franck / Chen, Zhe / Wiseman, John / Zhou, Shaoman / Liu, Peng / Salman, Mohammad / Verma, Kiran / Azadi, Niloufar / Downs-Bowen, Jessica / Tao, Sijia / Kumari, Amita / Zhang, Qingling / Smith, David B / Patel, Dharmeshkumar / Bassit, Leda / Schinazi, Raymond F

    Bioorganic chemistry

    2023  Volume 141, Page(s) 106923

    Abstract: Chronic hepatitis B virus (HBV) infection remains a major global health burden. It affects more than 290 million individuals worldwide and is responsible for approximately 900,000 deaths annually. Anti-HBV treatment with a nucleoside analog in ... ...

    Abstract Chronic hepatitis B virus (HBV) infection remains a major global health burden. It affects more than 290 million individuals worldwide and is responsible for approximately 900,000 deaths annually. Anti-HBV treatment with a nucleoside analog in combination with pegylated interferon are considered first-line therapy for patients with chronic HBV infection and liver inflammation. However, because cure rates are low, most patients will require lifetime treatment. HBV Capsid Assembly Modulators (CAMs) have emerged as a promising new class of compounds as they can affect levels of HBV covalently closed-circular DNA (cccDNA) associated with viral persistence. SAR studies around the core structure of lead HBV CAM GLP-26 (Fig. 1B) was performed and led to the discovery of non-toxic compound 10a displaying sub-nanomolar anti-HBV activity. Advanced toxicity and cellular pharmacology profiles of compounds 10a were also established and the results are discussed herein.
    MeSH term(s) Humans ; Capsid ; Hepatitis B virus ; Hepatitis B, Chronic/drug therapy ; Antiviral Agents/chemistry ; Capsid Proteins
    Chemical Substances Antiviral Agents ; Capsid Proteins
    Language English
    Publishing date 2023-10-20
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural
    ZDB-ID 120080-x
    ISSN 1090-2120 ; 0045-2068
    ISSN (online) 1090-2120
    ISSN 0045-2068
    DOI 10.1016/j.bioorg.2023.106923
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article: Discovery of a 2'-Fluoro,2'-Bromouridine Phosphoramidate Prodrug Exhibiting Anti-Yellow Fever Virus Activity in Culture and in Mice.

    LeCher, Julia C / Zandi, Keivan / Costa, Vivian Vasconcelos / Amblard, Franck / Tao, Sijia / Patel, Dharmeshkumar / Lee, Sujin / da Silva Santos, Felipe Rocha / Goncalves, Matheus Rodrigues / Queroz-Junior, Celso Martins / Marim, Fernanda Martins / Musall, Katie / Goh, Shu Ling / McBrayer, Tamara / Downs-Bowen, Jessica / De, Ramyani / Azadi, Niloufar / Kohler, James / Teixeira, Mauro Martins /
    Schinazi, Raymond F

    Microorganisms

    2022  Volume 10, Issue 11

    Abstract: Yellow fever virus (YFV) is a potentially lethal, zoonotic, blood-borne flavivirus transmitted to humans and non-human primates by mosquitoes. Owing to multiple deadly epidemics, the WHO classifies YFV as a "high impact, high threat disease" with ... ...

    Abstract Yellow fever virus (YFV) is a potentially lethal, zoonotic, blood-borne flavivirus transmitted to humans and non-human primates by mosquitoes. Owing to multiple deadly epidemics, the WHO classifies YFV as a "high impact, high threat disease" with resurgent epidemic potential. At present, there are no approved antiviral therapies to combat YFV infection. Herein we report on 2'-halogen-modified nucleoside analogs as potential anti-YFV agents. Of 11 compounds evaluated, three showed great promise with low toxicity, high intracellular metabolism into the active nucleoside triphosphate form, and sub-micromolar anti-YFV activity. Notably, we investigated a 2'-fluoro,2'-bromouridine phosphate prodrug (C9), a known anti-HCV agent with good stability in human blood and favorable metabolism. Predictive modeling revealed that C9 could readily bind the active site of the YFV RdRp, conferring its anti-YFV activity. C9 displayed potent anti-YFV activity in primary human macrophages, 3D hepatocyte spheroids, and in mice. In an A129 murine model, shortly after infection, C9 significantly reduced YFV replication and protected against YFV-induced liver inflammation and pathology with no adverse effects. Collectively, this work identifies a potent new anti-YFV agent with strong therapeutic promise.
    Language English
    Publishing date 2022-10-22
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2720891-6
    ISSN 2076-2607
    ISSN 2076-2607
    DOI 10.3390/microorganisms10112098
    Database MEDical Literature Analysis and Retrieval System OnLINE

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