Synthesis of C 2 Symmetric Potential Inhibitors of HIV-1 Protease From D-Mannitol |
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| Authors: | Gunilla Niklasson Ingemar Kvarnström Björn Classon Bertil Samuelsson? Ulrika Nillroth Helena Danielson |
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| Institution: | 1. Department of Chemistry , Link?ping University , S-581 83, Link?ping, Sweden;2. Department of Organic Chemistry , Arrhenius Laboratory Stockholm University , S-106 91, Stockholm, Sweden;3. Department of Biochemistry , Uppsala University BMC , S-751 23, Uppsala, Sweden |
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| Abstract: | ABSTRACT D-Mannitol was used as precursor for the synthesis of acyclic C 2 symmetric potential HIV-1 protease inhibitors. The 1- and 6-hydroxy groups of D-mannitol were substituted by -NHBoc, -NHValZ, -SAr, -SOAr and -SO2Ar and the 2-and 5-hydroxy groups were benzylated. In some products one of the central hydroxyl groups was either inverted or deoxygenated. Despite a close structural similarity to previously published inhibitors none of the products showed significant inhibitory activity against HIV-1 protease. |
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