PEPTIDES CONTAINING 2-FLUOROPHENYLALANINE, 3- OR 4-FLUOROPHENYLALANINE OR 2,2-DIFLUOROPHENYLALANINE 3,3-DIFLUOROPHENYLALANINE AS POTENTIAL INHIBITORS OF HIV PROTEASE
S. Viani et al., PEPTIDES CONTAINING 2-FLUOROPHENYLALANINE, 3- OR 4-FLUOROPHENYLALANINE OR 2,2-DIFLUOROPHENYLALANINE 3,3-DIFLUOROPHENYLALANINE AS POTENTIAL INHIBITORS OF HIV PROTEASE, Antiviral chemistry & chemotherapy, 6(1), 1995, pp. 65-72
A series of peptide mimetic substrates of the HIV-1 protease, correspo
nding substantially to the amino acid sequence of the Tyr-Pro cleavage
site contained in the gag polyprotein, in which the tyrosine amino ac
id of the scissile bond was replaced by 2-, 3- or 4-fluorophenylalanin
e or 2,2- or 3,3-difluorophenylalanine, has been developed. The synthe
sis of these compounds and the results of inhibition studies are descr
ibed.