Inhibitors of retroviral protease with a ketomethylene isosteric

Details Inhibitors of retroviral protease with a ketomethylene isosteric Inhibitors of retroviral protease with a ketomethylene isosteric

1991-02-07

1992-02-04

Lee, Lester L.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

6 to 7 amino acid residues in defined sequence

530330, A61K 3702, C07K 706

Patent

active

050861654

ABSTRACT:
Disclosed herein are compounds of the class of peptides having from about 4 to about 8 amino acid residues that are substrates for retroviral protease, e.g., HIV protease, derived from known cleavage sites and that are modified to contain an internal COCH.sub.2 bond isostere, useful as inhibitors of said retroviral protease, e.g., HIV protease, and exemplified by the modified peptide, Abz-Thr-Ile-Nle.PSI.(K)Nle-Gln-Arg-NH.sub.2, wherein K is COCH.sub.2.

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