Synthesis and Biological Activity of New Mixed HIV-Pr Inhibitors Conjugated to Bifunctional High Molecular Weight poly(Ethylene)glycol
| Autor: | Sara Drioli, Fabio Benedetti, Pietro Campaner, Federico Berti, Gian Maria Bonora |
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| Přispěvatelé: | Benedetti, Fabio, Berti, Federico, Bonora, GIAN MARIA, Campaner, Pietro, Drioli, Sara |
| Jazyk: | angličtina |
| Rok vydání: | 2011 |
| Předmět: |
Poly ethylene glycol
Organic Chemistry Human immunodeficiency virus (HIV) HIV Biological activity HIV Protease Catalytic site inhibitors dimerization inhibitors PEG Conjugated system dimerization inhibitor medicine.disease_cause Biochemistry Catalytic site inhibitor chemistry.chemical_compound chemistry PEG ratio medicine Organic chemistry Bifunctional |
| Zdroj: | ResearcherID |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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