Potent Cyclic Urea HIV Protease Inhibitors with 3-aminoindazole P2/P2' Groups

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 1999 Jan 1

PMID 9871528

Citations 5

Authors

J D Rodgers

B L Johnson

H Wang

R M Klabe

L Bacheler

B C Cordova

C H Chang

Affiliations

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Abstract

Cyclic ureas containing 3-aminoindazole P2/P2' groups are extremely potent inhibitors of HIV protease. The parent 3-aminoindazole 6 showed a Ki < 0.01 nM but poor translation of enzyme activity to antiviral activity was observed. A series of 3-alkylaminoindazoles revealed that translation improved with increasing lipophilicity. An X-ray crystal structure of 6 bound to HIV protease was obtained.

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