Increased antiviral activity of cyclic urea HIV protease inhibitors by modifying the P1/P1' substituents

R F Kaltenbach 3rd; R M Klabe; B C Cordova; S P Seitz

doi:10.1016/s0960-894x(99)00367-4

Increased antiviral activity of cyclic urea HIV protease inhibitors by modifying the P1/P1' substituents

Bioorg Med Chem Lett. 1999 Aug 2;9(15):2259-62. doi: 10.1016/s0960-894x(99)00367-4.

Authors

R F Kaltenbach 3rd¹, R M Klabe, B C Cordova, S P Seitz

Affiliation

¹ DuPont Pharmaceuticals Company, Experimental Station, Wilmington, DE 19880-0500, USA.

PMID: 10465557
DOI: 10.1016/s0960-894x(99)00367-4

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.

MeSH terms

Drug Design
HIV Protease Inhibitors / chemical synthesis*
HIV Protease Inhibitors / chemistry
HIV Protease Inhibitors / pharmacology
Structure-Activity Relationship
Urea / analogs & derivatives*
Urea / chemical synthesis
Urea / pharmacology

Substances

HIV Protease Inhibitors
Urea