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1. The synthesis and evaluation of cyclic ureas as HIV protease inhibitors: modifications of the P1/P1' residues.

Author

Patel M, Bacheler LT, Rayner MM, Cordova BC, Klabe RM, Erickson-Viitanen S, and Seitz SP

Subjects
Antiviral Agents chemistry, Antiviral Agents pharmacology, Azepines pharmacology, HIV drug effects, HIV Protease metabolism, HIV Protease Inhibitors chemistry, HIV Protease Inhibitors pharmacology, Indicators and Reagents, Kinetics, Molecular Structure, Structure-Activity Relationship, Urea chemistry, Urea pharmacology, Antiviral Agents chemical synthesis, HIV Protease Inhibitors chemical synthesis, Urea analogs & derivatives, Urea chemical synthesis
Abstract

Two series of cyclic ureas modified at the P1/P1' residue were prepared and evaluated for HIV protease inhibition and whole cell antiviral activity. Compounds 8b, 10 (3- and 4-pyridylmethyl analogs) and 6b (4-methoxy analog) showed significant improvement in antiviral activity relative to lead compounds DMP323 and DMP 450.

Published
1998
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