A Review of Strategies for the Development of Alkyl Prolines in Drug Discovery

Alessandra      Tolomelli; Alessandra      Ammazzalorso; Isabella      Bruno; Rosa      Amoroso

Abstract

Among all natural α-amino acids, proline represents a singularity. Due to the presence of the pyrrolidine ring, proline includes a secondary amino group, that does not contain a hydrogen atom when involved in an amide bond. A variety of synthetic analogues have been developed in the last years, based on ring substitutions, incorporation of heteroatoms into the ring, expansion or contraction of the pyrrolidine ring. The present review focuses on chemical synthesis of mono substituted derivatives of proline containing leucine, isoleucine, valine side chains, and other alkyls, including the contribution of literature from 2004 to 2015 or earlier where necessary.

Keywords: Alkyl proline, isoleucine, leucine, valine, proline chimera.

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Current Bioactive Compounds

Title:A Review of Strategies for the Development of Alkyl Prolines in Drug Discovery

Volume: 12 Issue: 3

Author(s): Alessandra Tolomelli, Alessandra Ammazzalorso, Isabella Bruno and Rosa Amoroso

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Keywords: Alkyl proline, isoleucine, leucine, valine, proline chimera.

Abstract: Among all natural α-amino acids, proline represents a singularity. Due to the presence of the pyrrolidine ring, proline includes a secondary amino group, that does not contain a hydrogen atom when involved in an amide bond. A variety of synthetic analogues have been developed in the last years, based on ring substitutions, incorporation of heteroatoms into the ring, expansion or contraction of the pyrrolidine ring. The present review focuses on chemical synthesis of mono substituted derivatives of proline containing leucine, isoleucine, valine side chains, and other alkyls, including the contribution of literature from 2004 to 2015 or earlier where necessary.

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Tolomelli Alessandra, Ammazzalorso Alessandra, Bruno Isabella and Amoroso Rosa, A Review of Strategies for the Development of Alkyl Prolines in Drug Discovery, Current Bioactive Compounds 2016; 12 (3) . https://dx.doi.org/10.2174/1573407212666160511155230

DOI https://dx.doi.org/10.2174/1573407212666160511155230	Print ISSN 1573-4072
Publisher Name Bentham Science Publisher	Online ISSN 1875-6646