Synthesis and biological activity of potent HIV-1 protease inhibitors based on Phe-Pro dihydroxyethylene isosteres

F Benedetti, F Berti, S Budal, P Campaner…

文献索引：Benedetti, Fabio; Berti, Federico; Budal, Sara; Campaner, Pietro; Dinon, Francesca; Tossi, Alessandro; Argirova, Radka; Genova, Petia; Atanassov, Vasil; Hinkov, Anton Journal of Medicinal Chemistry, 2012 , vol. 55, # 8 p. 3900 - 3910

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被引用次数: 11

摘要

Peptidomimetic inhibitors of HIV-1 PR are still a key resource in the fight against AIDS. Here we describe the synthesis and biological activity of HIV-1 PR inhibitors based on four novel dihydroxyethylene isosteres of the Phe-Pro and Pro-Pro dipeptides. The isosteres, containing four stereogenic centers, were synthesized in high yield and excellent stereoselectivity via the cyclization of epoxy amines derived from α-amino acids. The ...