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 and cell permeability. Low nanomolar activity and synergism were obtained by coupling a Phenylalanine – Proline pseudopeptide catalytic site inhibitor and the Val-Val-Phe tripeptide dimerization inhibitor.

Synthesis and Biological Activity of New Mixed HIV-Pr Inhibitors Conjugated to Bifunctional High Molecular Weight poly(Ethylene)glycol

BENEDETTI, FABIO;BERTI, FEDERICO;BONORA, GIAN MARIA;CAMPANER, PIETRO;DRIOLI, Sara
2011-01-01

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 and cell permeability. Low nanomolar activity and synergism were obtained by coupling a Phenylalanine – Proline pseudopeptide catalytic site inhibitor and the Val-Val-Phe tripeptide dimerization inhibitor.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11368/2356934
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