European Journal of Medicinal Chemistry p. 423 - 436 (1998)
Update date:2022-08-05
Topics: Synthesis Inhibitors Catalyst Purification Reaction Conditions Activity Biological assay HIV protease
Garrouste, Patrick
Pawlowski, Macek
Tonnaire, Thierry
Sicsic, Sames
Dumy, Pascal
De Rosny, Eve
Reboud-Ravaux, Michele
Fulcrand, Pierre
Martinez, Jean
We report here the synthesis and activity of HIV protease inhibitors. In 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 carboxylic 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/activity study of a peptide substrate. These modifications allowed us to work up the synthesis of new pseudopeptide bonds: amino-amide and hydroxy-amide. Compounds with activity in the micromolar range were actually a starting point for the synthesis of new protease inhibitors.
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