Non-peptide-based inhibitors of human immunodeficiency virus-1 protease

The use of bis(α-aminoalkyl)phosphinic acids as analogs of the tetrahedral intermediate formed on the path to peptide hydrolysis in combination with a mimic for a structural water, which is found in HIV protease inhibitor complexes, leads to potent inhibitors of HIV-1 protease. The use of bis(α-amin...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1994-11, Vol.4 (21), p.2601-2604
Main Authors: Peyman, Anusch, Stahl, Wilhelm, Wagner, Konrad, Ruppert, Dieter, Budt, Karl-Heinz
Format: Article
Language:English
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Summary:The use of bis(α-aminoalkyl)phosphinic acids as analogs of the tetrahedral intermediate formed on the path to peptide hydrolysis in combination with a mimic for a structural water, which is found in HIV protease inhibitor complexes, leads to potent inhibitors of HIV-1 protease. The use of bis(α-aminoalkyl)phosphonic acids as analogs of the tetrahedral intermediate formed on the path to peptide hydrolysis in combination with a mimic for a structural water, whihc is found in HIV protease inhibitor complexes, leads to potent inhibitors of HIV-1 protease.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)80292-4