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.
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Authors | W W Wilkerson, E Akamike, W W Cheatham, A Y Hollis, R D Collins, I DeLucca, P Y Lam, Y Ru |
Journal | Journal of medicinal chemistry
(J Med Chem)
Vol. 39
Issue 21
Pg. 4299-312
(Oct 11 1996)
ISSN: 0022-2623 [Print] United States |
PMID | 8863807
(Publication Type: Journal Article)
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Chemical References |
- Anti-HIV Agents
- Benzamides
- HIV Protease Inhibitors
- RNA, Viral
- Urea
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Topics |
- Anti-HIV Agents
(chemistry, pharmacology)
- Benzamides
(chemistry, pharmacology)
- Chromatography, High Pressure Liquid
- HIV Protease Inhibitors
(chemistry)
- HIV-1
(drug effects, enzymology, physiology)
- Kinetics
- RNA, Viral
(metabolism)
- Structure-Activity Relationship
- Urea
(analogs & derivatives, pharmacology)
- Virus Replication
(drug effects)
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