Office of Technology Transfer – University of Michigan

2.2-BIS-(HYDROXYMETHYL) Cyclopropylidenemethylpurines and - Pyrimidines as Antiviral Agents

Technology #2337

Background

Viruses are the etiologic cause of many life-threatening human diseases. Of special importance are herpes viruses such as herpes simplex 1 (HSV-1), herpes simplex virus 2 (HSV-2) , cytomegalovirus (CMV0, Epstein-Barr virus (EBV), varicella zoster virus (VZV) and human herpes viruses 6,7, and 8 (HHV-6,-7,-8) which are associated with many common viral illnesses. Various derivatives of nuceloside analogues have been foung to exhibit antiviral activity. Notably, acyclovir (Zovirax) and its prodrug valacyclovir (Valtrex) are approved for infections caused by HSV-1 and HSV-2. However, there continues to be a need for novel compounds that are active against pathogenic viruses.

Technology

University of Michigan researchers in collaboration with the “Karmanos Cancer Institute” have discovered novel 2,2-bis-(hydroxymethyl)cyclopropylidenemethyl derivatives and heterocyclic compounds, prodrugs, and pharmacologically acceptable salts thereof. The compounds are useful as antiviral agents and are effective against HCMV, HSV-1, HSV-2, HIV, EBV and HBV, as well as against other mammalian viruses.

Applications and Advantages

Applications

  • Novel antivirals against HCMV, HSV-1, HSV-2, HIV, EBV and HBV.

Advantages

  • The effects against HCMV were stronger-nl-than ganciclovir, the current leading drug-nl-of choice for HCMV.
  • Tests showed complete lack of cytotoxicity-nl-for cells that have no viral activity.