A series of peptide mimetic substrates of the HIV-1 protease, corresponding substantially to the amino acid sequence of the Tyr-Pro cleavage site contained in the gag polyprotein, in which the tyrosine amino acid of the scissile bond was replaced by 2-, 3- or 4-fluorophenylalanine or 2,2- or 3,3-difluorophenylalanine, has been developed. The synthesis of these compounds and the results of inhibition studies are described.
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