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Stereocontrolled synthesis and biological activity of two diastereoisomers of the potent HIV-1 protease inhibitor saquinavir.

Righi G, Ciambrone S, Bonini C, Campaner P

Istituto di Chimica Biomolecolare-Sezione di Roma, c/o Dipartimento di Chimica, Università La Sapienza, p.le A. Moro 5, 00185 Roma, Italy. giuliana.righi@uniroma1.it

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.

Published 1 February 2008 in Bioorg Med Chem, 16(2): 902-8.
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