New benzophenone phosphonate derivatives

What is it about?

A set of benzophenones is known to posses anti-HIV activity thanks to binding in the hydrophobic pocket of the Reverse Transcriptase enzyme. We have modified these compounds with the phoshonate residue in order to improve solubility and retain its potential antiviral activity

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Why is it important?

Low solubility of pharmacologically active compounds in medicinal chemistry is a big problem. Since most of preclinical and clinical studies deal with the substance itself (not with a final prescribing form of a gelatine pill or emulsion), much efforts are brought to create compounds in balance with lypophylicity, needed for proper binding in the proteins' active sites, and with water solubility, needed for accurate investigtion of bioactivity and cytotoxicity.

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