ANTI-HIV CARBONUCLEOSIDE PHOSPHONATES

Development of a phosphonate carbonucleoside presenting very significant activity on the AIDS virus in cell cultures.

Context
Acquired immunodeficiency syndrome (AIDS) is one of the leading causes of death in the world. While combined therapies, such as anti-retroviral therapy (highly active antiretroviral therapy – HAART), have contributed significantly to virus elimination and have improved quality of life for people, problems such as intolerance and the emergence of resistance among members of particular classes of pharmaceutical drugs remain a major problem for successful long-term treatment. As a result, there is an ongoing need for new anti-HIV drugs with greater power and improved pharmacokinetic properties.

Benefits
The originality of this project’s invention resides in the non-natural L configuration of designed carbocyclic phosphonate nucleosides. The use of L-nucleoside analogs as antiviral agents leads to an antiviral activity that is comparable, and sometimes better than, their D counterparts, along with a more favorable toxicolgical profile and better metabolic stability.

Applications
Chemotherapy for HIV and other infectious diseases in which nucleoside analogs have been identified as antiviral drugs.