A self-assembling HIV protease inhibitor (Meeting abstract). NLM AIDSLINE Important note: Information in this article was accurate in 1993. The state of the art may have changed since the publication date.

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A self-assembling HIV protease inhibitor (Meeting abstract).

Proc Annu Meet Am Assoc Cancer Res; 34:A1674 1993. Unique Identifier : AIDSLINE ICDB/93692614
Chiang LC C; Derango R; Rideout D; Dept. of Molecular Biology, Scripps Res. Inst., La Jolla, CA; 92037

Abstract: As part of an ongoing program to create antiretroviral prodrug combinations with low mol wt and high membrane permeabilities, we have developed a combination of an aldehyde A and an acylhydrazide B. An equimolar combination inhibits HIV protease with EC90 = 160 uM each, as compared to EC90 greater than or equal to 2000 uM for either A or B alone. Proton NMR and mass spectroscopy suggest that the synergistic inhibition by A + B is due to equilibrium with C, which resembles potent HIV protease inhibitors such as L-682-679 (DeSolms et al, J Med Chem 34:2852, 1991). The chemical structures for A, B and C are diagrammed.
Keywords: Cell Membrane Permeability *HIV Protease Inhibitors/CHEMISTRY/PHARMACOKINETICS Nuclear Magnetic Resonance Prodrugs Spectrum Analysis, Mass ABSTRACTKWDcellmembranepermeabilityKWDhivproteaseinhibitors/chemistry/pharmacokineticsnuclearmagneticresonanceprodrugsspectrumanalysis,massabstract
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Copyright © 1993 - National Library of Medicine. Reproduced under license with the National Library of Medicine, Bethesda, MD.

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