Synthesis and Biological Activity of New Mixed HIV-PR Inhibitors Conjugated to Bifunctional High-Molecular Weight Poly(Ethylene Glycol)

We have synthesized and evaluated a small set of dual action HIV-Protease inhibitors, consisting of a catalytic site reversible inhibitor conjugated with a dimerization peptidic inhibitor, linked via a suitable selective end-modified poly(ethylene glycol), in an effort to obtain a synergistic effect with improved biological behaviour and more powerful pharmacological features, such as water solubility, cell permeability and bioavailability.