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

Abstract:

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.

Autoren:   Benedetti, Fabio; Berti, Federico; M Bonora, Gian; Campaner, Pietro; Drioli, Sara
Journal:   Letters in Organic Chemistry
DOI:   10.2174/157017811796064421
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