Phosphorus AIDS HIV users

Innovative minds gathered in Birmingham in mid-July for the Rhodia sponsored 16th International Conference on Phosphorus Chemistry to hear scientists debating the significance of phosphorus in today's world - from its major influence on biological evolution to its role as a vital ingredient in drugs to combat AIDS.

The main focus on applications in medicinal chemistry was the Gilead Symposium on Antiviral Chemistry. The symposium offered delegates the chance to hear leading phosphorus chemistry experts Czech chemist, Dr Tony Holy, and Belgian doctor, Professor Erik de Clercq tell the story of how their research partnership led to the discovery of tenofovir, the active ingredient in Viread, the antiretroviral HIV drug from US drug company Gilead.

Subsequent to that there were speakers present-ing current pro-drug strategies involving phosphorus, including a paper from Karl Hostetler from the department of medicine, San Diego Healthcare System. He said that while tenofovir, adefovir and cidofovir have been successfully developed as potent antiviral therapies for viral diseases including AIDS, Hep B and CMV, they are not generally well absorbed from the GI tract.

He said that to make cidofovir orally active, they used a design paradigm drawn from lipid absorption in the GI tract, preparing analogues of cidofovir which are related to lysophosphatidylcholine, a naturally occurring dietary phospholipid. The resulting compound is 100 fold more active against cowpox and smallpox than unmodified cidofovir in vitro. Hostetler said they believed this approach is generally applicable