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J Med Chem. 1991 Sep;34(9):2852-7.

Design and synthesis of HIV protease inhibitors. Variations of the carboxy terminus of the HIV protease inhibitor L-682,679.

Author information

1
Merck Sharp & Dohme Research Laboratories, West Point, Pennsylvania 19486.

Abstract

A series of tetrapeptide analogues of 1 (L-682,679), in which the carboxy terminus has been shortened and modified, was prepared and their inhibitory activity measured against the HIV protease in a peptide cleavage assay. Selected examples were tested as inhibitors of virus spread in cell culture. Compound 12 was a 10-fold more potent enzyme inhibitor than 1 in vitro and 30-fold more potent in inhibiting the viral spread in cells.

PMID:
1910089
DOI:
10.1021/jm00113a025
[Indexed for MEDLINE]

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