Potent Inhibitors of the HIV-1 Protease with Good Oral Bioavailabilities

A series of novel pseudo-symmetrical and unsymmetrical inhibitors based on the backbone modification of a peptidomimetic were synthesized and found to be highly potent inhibitors of the HIV-1 protease (IC50 = 2.9 to

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Bibliographic Details
Published in:Biochemical and biophysical research communications 1995-06, Vol.211 (1), p.159-165
Main Authors: Sham, H.L., Zhao, C., Marsh, K.C., Betebenner, D.A., Lin, S.Q., Mcdonald, E., Vasavanonda, S., Wideburg, N., Saldivar, A., Robins, T., Kempf, D.J., Plattner, J.J., Norbeck, D.W.
Format: Article
Language:English
Subjects:
AIDS/HIV
Animals
Biological Availability
Dogs
Drug Design
Female
HIV Protease - metabolism
HIV Protease Inhibitors - chemical synthesis
HIV Protease Inhibitors - pharmacokinetics
HIV Protease Inhibitors - pharmacology
Indicators and Reagents
Macaca fascicularis
Male
Metabolic Clearance Rate
Molecular Structure
Rats
Rats, Sprague-Dawley
Structure-Activity Relationship
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Description
Summary:A series of novel pseudo-symmetrical and unsymmetrical inhibitors based on the backbone modification of a peptidomimetic were synthesized and found to be highly potent inhibitors of the HIV-1 protease (IC50 = 2.9 to
ISSN:0006-291X
1090-2104
DOI:10.1006/bbrc.1995.1791