Abstract
A series of N,N'-disubstituted cyclic urea 3-benzamides has been synthesized and evaluated for HIV protease inhibition and antiviral activity. Some of these benzamides have been shown to be potent inhibitors of HIV protease with Ki < 0.050 nM and IC90 < 20 nM for viral replication and, as such, may be useful in the treatment of AIDS. The synthesis and quantitative structure-activity relationship for this benzamide series will be discussed.
MeSH terms
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Anti-HIV Agents / chemistry*
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Anti-HIV Agents / pharmacology
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Benzamides / chemistry*
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Benzamides / pharmacology
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Chromatography, High Pressure Liquid
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HIV Protease Inhibitors / chemistry*
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HIV-1 / drug effects
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HIV-1 / enzymology
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HIV-1 / physiology
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Kinetics
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RNA, Viral / metabolism
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Structure-Activity Relationship
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Urea / analogs & derivatives*
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Urea / pharmacology
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Virus Replication / drug effects
Substances
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Anti-HIV Agents
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Benzamides
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HIV Protease Inhibitors
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RNA, Viral
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Urea