Synthesis and antiviral evaluation of novel heteroarylpyrimidines analogs as HBV capsid effectors |
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| Authors: | Sebastien Boucle Xiao Lu Leda Bassit Tugba Ozturk Olivia Ollinger Russell Franck Amblard Steven J. Coats Raymond F. Schinazi |
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| Affiliation: | 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 |
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| Abstract: | New modifications to the scaffold of previously reported HBV capsid assembly effectors such as BAY 41-4109, HAP-12 and GLS4 were explored. The anti-HBV activity in the HepAD38 system, and cytotoxicity profiles of each of the new compounds has been assessed. Among them, five new iodo- and bromo-heteroarylpyrimidines analogs displayed anti-HBV activity in the low micromolar range. |
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| Keywords: | HBV HAP Heteroarylpyrimidine Capsid assembly effectors |
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