The patent describes new peptidomimetic inhibitors of retroviral proteases, in particular of human immunodeficiency virus (HIV) protease. These inhibitors comprise as the core structure a new diaminodiol isostere of the dipeptide Phe-Pro having four stereogenic centres. The inhibitors of the invention have been shown to inhibit HIV protease and can therefore be usefully employed as antivirals for post-exposure prophylaxis and as a therapy for viral infections by a retrovirus, in particular HIV. The syntheses processes of the isosteres and inhibitors are also described.
PEPTIDOMIMETIC INHIBITORS OF RETROVIRAL PROTEASES AND THEIR USE AS ANTIVIRALS / Benedetti, Fabio; Tossi, Alessandro; Berti, Federico; Campaner, Pietro; Dinon, F.. - STAMPA. - (2005).
PEPTIDOMIMETIC INHIBITORS OF RETROVIRAL PROTEASES AND THEIR USE AS ANTIVIRALS
BENEDETTI, FABIO;TOSSI, ALESSANDRO;BERTI, FEDERICO;CAMPANER, PIETRO;
2005-01-01
Abstract
The patent describes new peptidomimetic inhibitors of retroviral proteases, in particular of human immunodeficiency virus (HIV) protease. These inhibitors comprise as the core structure a new diaminodiol isostere of the dipeptide Phe-Pro having four stereogenic centres. The inhibitors of the invention have been shown to inhibit HIV protease and can therefore be usefully employed as antivirals for post-exposure prophylaxis and as a therapy for viral infections by a retrovirus, in particular HIV. The syntheses processes of the isosteres and inhibitors are also described.Pubblicazioni consigliate
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