Small hydroxyethylene-based peptidomimetics inhibiting both HIV-1 and C. albicans aspartic proteases

A Tossi, F Benedetti, S Norbedo, D Skrbec…

文献索引：Tossi, Alessandro; Benedetti, Fabio; Norbedo, Stefano; Skrbec, Damiano; Berti, Federico; Romeo, Domenico Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 22 p. 4719 - 4727

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被引用次数: 33

摘要

We have extended a highly flexible method for rapidly assembling aspartic protease inhibitors to produce symmetric and asymmetric monohydroxyethylene peptidomimetics. This method is based on the prior synthesis of the central non-cleavable peptide-bond isostere [NH2–P1ψP1′–NH2; ψ= hydroxyethylene isostere, HNCH (Bz) CHOHCH2CH (Bz) NH], with the possibility of accurately controlling its stereochemistry (S, S, S or S, R, S), ...