FLUORINATED ANALOGS OF THE P17 P24 SEQUENCE INCORPORATING 3-FLUORO AND 3,3-DIFLUORO PHENYLALANINES AS POTENTIAL INHIBITORS OF HIV PROTEASE/

The synthesis and activity of a series of fluorinated peptide analogue s of the p17/p24 sequence incorporating 3-fluoro and 3,3-difluoro phen ylananines at the P-1 position of the scissile bond are described. It was hoped that these might act as potent inhibitors of HIV protease. I n fact, none of the compounds studied displayed any anti-HIV activity in vitro. This may be attributed to poor cell penetration of the compo unds and metabolic cleavage of their peptide bonds.