We report here the synthesis and activity of HIV protease inhibitors.
Ln the first stage hydrophobic compounds incorporating a 'carba' bond
surrogate or a beta-homologated residue were synthesized. Secondly, we
synthesized cyclic compounds in which we incorporated 2-quinoline car
boxylic acid in the P3 position and the amino-hydroxyindane moiety in
the P'3. The last part of this work was dedicated to a structure/activ
ity study of a peptide substrate. These modifications allowed us to wo
rk up the synthesis of new pseudopeptide bonds: amino-amide and hydrox
y-amide, Compounds with activity in the micromolar range were actually
a starting point for the synthesis of new protease inhibitors. (C) El
sevier, Paris.