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Antiviral activity of novel 2'-fluoro-6'-methylene-carbocyclic adenosine against wild-type and drug-resistant hepatitis B virus mutants |
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| Authors: | Wang Jianing Singh Uma S Rawal Ravindra K Sugiyama Masaya Sugiyama Massaya Yoo Jakyung Jha Ashok K Scroggin Melissa Huang Zhuhui Murray Michael G Govindarajan Rajgopal Tanaka Yasuhito Korba Brent Chu Chung K |
| Institution: | The University of Georgia, College of Pharmacy, Athens, GA 30602, USA. |
| Abstract: | Novel 2'-fluoro-6'-methylene-carbocyclic adenosine (9) was synthesized and evaluated its anti-HBV activity. The titled compound demonstrated significant antiviral activity against wild-type as well as lamivudine, adefovir and double lamivudine/entecavir resistant mutants. Molecular modeling study indicate that the 2'-fluoro moiety by a hydrogen bond, as well as the van der Waals interaction of the carbocyclic ring with the phenylalanine moiety of the polymerase promote the positive binding, even in the drug resistant mutants. |
| Keywords: | Carbocyclic nucleoside anti-HBV Drug-resistant |
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