PYROGLUTAMIC ACID DERIVATIVES: BUILDING BLOCKS FOR DRUG DISCOVERY

被引：19

作者：

Stefanucci, Azzurra ^{[1
]}

Novellino, Ettore ^{[2
]}

Costante, Roberto ^{[3
]}

Mollica, Adriano ^{[3
]}

机构：

[1] Univ Rome, Dipartimento Chim, I-00187 Rome, Italy

[2] Univ Naples Federico II, Dipartimento Farm, I-80131 Naples, Italy

[3] Univ Chieti Pescara G dAnnunzio, Dipartimento Farm, I-66100 Chieti, Italy

来源：

HETEROCYCLES | 2014年 / 89卷 / 08期

关键词：

Pyroglutamic Acid; Proline Chimera; Peptide; Asymmetric Synthesis; Peptidomimietic; ALPHA-AMINO-ACIDS; MICHAEL ADDITION-REACTIONS; VIRTUALLY COMPLETE CONTROL; RESTRICTED TRH ANALOGS; ENANTIOSELECTIVE SYNTHESIS; ASYMMETRIC-SYNTHESIS; GLUTAMIC-ACID; NUCLEOPHILIC GLYCINE; N-BENZYL-2,3-O-ISOPROPYLIDENE-D-GLYCERALDEHYDE NITRONE; 1,3-DIPOLAR CYCLOADDITION;

D O I：

10.3987/REV-14-800

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Substituted prolines namely amino acid proline chimeras, have received a great synthetic efforts with the aim to develop a full library of compounds to be used in bioactive peptides drug discovery. Conversely pyroglutamic acid derivatives, strictly related to proline chimeras have been used only marginally in peptide modifications, probably due the lack of handled asymmetric syntheses. In this work we reviewed the "state of the art" on the synthetic approaches to pyroglutamic acid derivatives bearing a side chain related to that of natural amino acids.

引用

页码：1801 / 1825

页数：25

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