2. Academic Validation
  3. Antiviral activity of novel 2'-fluoro-6'-methylene-carbocyclic adenosine against wild-type and drug-resistant hepatitis B virus mutants

Antiviral activity of novel 2'-fluoro-6'-methylene-carbocyclic adenosine against wild-type and drug-resistant hepatitis B virus mutants

  • Bioorg Med Chem Lett. 2011 Nov 1;21(21):6328-31. doi: 10.1016/j.bmcl.2011.08.113.
Jianing Wang 1,  Uma S Singh,  Ravindra K Rawal,  Masaya Sugiyama,  Jakyung Yoo,  Ashok K Jha,  Melissa Scroggin,  Zhuhui Huang,  Michael G Murray,  Rajgopal Govindarajan,  Yasuhito Tanaka,  Brent Korba,  Chung K Chu
Affiliations

Affiliation

  • 1 The University of Georgia, College of Pharmacy, Athens, GA 30602, USA.
PMID: 21930377 DOI: 10.1016/j.bmcl.2011.08.113
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.

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