title: Increased antiviral activity of cyclic urea HIV protease inhibitors by modifying the P1/P1' substituents.
abstract: A series of alkyl substituted P1/P1' analogs was prepared in an attempt to increase translation of the 3-aminoindazole class of HIV protease inhibitors. Increasing the lipophilicity of the P1/P1' residues dramatically improved translation of enzyme activity to antiviral activity in the whole cell assay.
authors.affiliation: DuPont Pharmaceuticals Company, Experimental Station, Wilmington, DE 19880-0500, USA.
authors.forename: R F
authors.initials: RF
authors.lastname: Kaltenbach
authors.forename: R M
authors.initials: RM
authors.lastname: Klabe
authors.forename: B C
authors.initials: BC
authors.lastname: Cordova
authors.forename: S P
authors.initials: SP
authors.lastname: Seitz
mesh_terms: D015195:Drug Design; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014508:Urea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D017320:HIV Protease Inhibitors; D014508:Urea