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HIV protease inhibitory bis-benzamide cyclic ureas: a quantitative structure-activity relationship analysis.

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.
AuthorsW W Wilkerson, E Akamike, W W Cheatham, A Y Hollis, R D Collins, I DeLucca, P Y Lam, Y Ru
JournalJournal of medicinal chemistry (J Med Chem) Vol. 39 Issue 21 Pg. 4299-312 (Oct 11 1996) ISSN: 0022-2623 [Print] United States
PMID8863807 (Publication Type: Journal Article)
Chemical References
  • Anti-HIV Agents
  • Benzamides
  • HIV Protease Inhibitors
  • RNA, Viral
  • Urea
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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