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Bioorg Med Chem. 2008 Jan 15;16(2):902-8. Epub 2007 Oct 12.

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

Author information

1
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

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.

PMID:
17964171
DOI:
10.1016/j.bmc.2007.10.020
[Indexed for MEDLINE]

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