SAR studies in the sulfonyl carboxamide class of HBV capsid assembly modulators |
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| Affiliation: | 1. Laboratory of Immunopharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China;2. Chinese National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China;3. Tongji Hospital of Tongji Medical College, Wuhan, China;1. Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA;2. Cocrystal Pharma, Inc., 1860 Montreal Road, Tucker, GA 30084, USA;1. Department of Medicinal Chemistry, Key Laboratory of Chemical Biology, Ministry of Education, School of Pharmaceutical Sciences, Shandong University, Jinan, 250012, China;2. Department of Molecular Microbiology and Immunology, Saint Louis University School of Medicine, St. Louis, MO, USA;3. Saint Louis University Liver Center, Saint Louis University School of Medicine, St. Louis, MO, USA;4. Centro de Biología Molecular “Severo Ochoa” (Consejo Superior de Investigaciones Científicas & Universidad Autónoma de Madrid), Madrid, Spain |
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| Abstract: | The HBV core protein has multiple essential functions in the HBV life cycle to enable chronic HBV infection. The core protein oligomerizes to form the viral capsid, and modulation of the HBV capsid assembly process has shown clinical efficacy in early clinical trials. Herein is described the SAR exploration of NVR 3-778, the first clinical compound in the sulfonyl carboxamide class. |
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| Keywords: | HBV Core protein Capsid modulator Sulfonamide |
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