Affiliation:
1. Institute of Molecular Medicine, Feinstein Institutes for Medical Research, Manhasset, NY, USA
Abstract
Abstract:
For over 50 years of azapeptide synthetic techniques, developments have renewed
the field of peptidomimetic therapeutics. Azapeptides are close surrogates of natural peptides:
they contain a substitution of the amino acid α-carbon by a nitrogen atom. Goserelin
(1989) and Atazanavir (2003) are two well-known, FDA-approved azapeptide-based drugs
for the treatment of cancers and HIV infection, providing evidence for the successful clinical
implementation of this class of therapeutic. This review highlights the azapeptides in recent
medicinal chemistry applications and synthetic milestones. We describe the current techniques
for azapeptide bond formation by introducing azapeptide coupling reagents and chain
elongation methods both in solution and solid-phase strategies.
Publisher
Bentham Science Publishers Ltd.
Subject
Pharmacology,Molecular Medicine,Drug Discovery,Biochemistry,Organic Chemistry
Cited by
4 articles.
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