Orally bioavailable anti-HBV dinucleotide acyloxyalkyl prodrugs

  • Bioorg Med Chem Lett. 2010 Mar 1;20(5):1783-6. doi: 10.1016/j.bmcl.2010.01.010.
John E Coughlin  1 ,  Seetharamaiyer Padmanabhan ,  Guangrong Zhang ,  Cassandra J Kirk ,  Chandrika P Govardhan ,  Brent E Korba ,  Kathleen O'Loughlin ,  Carol E Green ,  Jon Mirsalis ,  John D Morrey ,  Radhakrishnan P Iyer
Affiliations
  • 1. Spring Bank Pharmaceuticals Inc., Milford, MA, United States.
Abstract

The acyloxyalkyl derivatives of a model anti-HBV dinucleotide were synthesized and evaluated as orally bioavailable prodrugs. Our studies have led to the identification of the first orally bioavailable dinucleotide prodrugs for further therapeutic development against the hepatitis B virus (HBV).