title: 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.
authors.affiliation: DuPont Merck Pharmaceutical Company, E500/3203 Experimental Station, Wilmington, Delaware 19880-0500, USA.
authors.forename: W W
authors.initials: WW
authors.lastname: Wilkerson
authors.forename: E
authors.initials: E
authors.lastname: Akamike
authors.forename: W W
authors.initials: WW
authors.lastname: Cheatham
authors.forename: A Y
authors.initials: AY
authors.lastname: Hollis
authors.forename: R D
authors.initials: RD
authors.lastname: Collins
authors.forename: I
authors.initials: I
authors.lastname: DeLucca
authors.forename: P Y
authors.initials: PY
authors.lastname: Lam
authors.forename: Y
authors.initials: Y
authors.lastname: Ru
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry* / Q000494:pharmacology; D001549:Benzamides / Q000737:chemistry* / Q000494:pharmacology; D002851:Chromatography, High Pressure Liquid; D017320:HIV Protease Inhibitors / Q000737:chemistry*; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology / Q000502:physiology; D007700:Kinetics; D012367:RNA, Viral / Q000378:metabolism; D013329:Structure-Activity Relationship; D014508:Urea / Q000031:analogs & derivatives* / Q000494:pharmacology; D014779:Virus Replication / Q000187:drug effects
chemical_list: D019380:Anti-HIV Agents; D001549:Benzamides; D017320:HIV Protease Inhibitors; D012367:RNA, Viral; D014508:Urea