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

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

Volume: 8 Issue: 6

Author(s): Fabio Benedetti, Federico Berti, Gian M. Bonora, Pietro Campaner and Sara Drioli

Affiliation:

Keywords: Poly(ethylene glycol), HIV-PR inhibitors, mixed conjugates, permeability, bioavailability, synergistic, pseudopeptide, dimerization inhibitors, aromatic groups, Oligopeptides

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.

Cite this article as:

Benedetti Fabio, Berti Federico, M. Bonora Gian, Campaner Pietro and Drioli Sara, Synthesis and Biological Activity of New Mixed HIV-PR Inhibitors Conjugated to Bifunctional High-Molecular Weight Poly(Ethylene Glycol), Letters in Organic Chemistry 2011; 8 (6) . https://dx.doi.org/10.2174/157017811796064421