Increased antiviral activity of cyclic urea HIV protease inhibitors by modifying the P1/P1' substituents.
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.
Kaltenbach
R F
RF
DuPont Pharmaceuticals Company, Experimental Station, Wilmington, DE 19880-0500, USA.
Klabe
R M
RM
Cordova
B C
BC
Seitz
S P
SP
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
D017320:HIV Protease Inhibitors; D014508:Urea