A general enantioselective synthesis of new syn-hydroxyethylamine isosteres has been developed. The approach, based on the controlled opening of functionalized optically active 2,3-epoxy amines, can be conveniently used for the preparation of new peptidomimetics with various residues. Finally the total synthesis of two diastereoisomer analogues of HIV-Protease inhibitor Saquinavir has been achieved and their biological activity evaluated. (C) 2007 Elsevier Ltd. All rights reserved.
Stereocontrolled Synthesis and Biological Activity of two Diastereoisomers of the Potent HIV-1 Protease Inhibitor Saquinavir
Righi G;
2007
Abstract
A general enantioselective synthesis of new syn-hydroxyethylamine isosteres has been developed. The approach, based on the controlled opening of functionalized optically active 2,3-epoxy amines, can be conveniently used for the preparation of new peptidomimetics with various residues. Finally the total synthesis of two diastereoisomer analogues of HIV-Protease inhibitor Saquinavir has been achieved and their biological activity evaluated. (C) 2007 Elsevier Ltd. All rights reserved.File in questo prodotto:
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