New dipeptide isosteres useful for the inhibition of HIV-1 protease

A family of readily accessible Phe-Pro mimics has been devised in which ortho-substituted benzamides serve as proline surrogates. When suitably functionalized, these dipeptide isosteres afford potent inhibitors of HIV-1 protease which are also effective in whole cell antiviral assays. A family of re...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 4; no. 11; pp. 1385 - 1390
Main Authors Kaldor, Stephen W., Hammond, Maryls, Dressman, Bruce A., Fritz, James E., Crowell, Thomas A., Hermann, Robert A.
Format Journal Article
LanguageEnglish
Published Oxford Elsevier Ltd 09.06.1994
Elsevier
Subjects
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Biological and medical sciences
Medical sciences
Pharmacology. Drug treatments
Virus
Structure activity relation
HIV-1 virus
Enzyme
Retroviridae
Dipeptides
Enzyme inhibitor
Hydrolases
Lentivirinae
Antiviral
Human immunodeficiency virus
Proteinases
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Summary:A family of readily accessible Phe-Pro mimics has been devised in which ortho-substituted benzamides serve as proline surrogates. When suitably functionalized, these dipeptide isosteres afford potent inhibitors of HIV-1 protease which are also effective in whole cell antiviral assays. A family of readily accessible Phe-Pro mimics has been devised in which ortho-substituted benzamides serve as proline surrogates. When suitably functionalized, these dipeptide isosteres afford potent inhibitors of HIV-1 protease which are also effective in whole cell antiviral assays.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)80367-X