The Application of Freidinger Lactams and their Analogs in the Design of Conformationally Constrained Peptidomimetics

Author(s): Andrej Perdih, Danijel Kikelj

Journal Name: Current Medicinal Chemistry

Volume 13 , Issue 13 , 2006

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Peptides exist in solution as an equilibrium mixture of conformers. The backbone conformational constraints are of interest as a means of limiting degrees of freedom and thereby constraining a synthetic peptide into the bioactive conformation. This concept plays an important role in the design of peptidomimetics in the drug development process. In the early eighties, Freidinger proposed the concept of protected lactam-bridged dipeptides, which was a milestone in the design of conformationally constrained peptides. These types of compounds, now widely known as Freidinger lactams, have been of interest to many medicinal and peptide chemists. This review seeks to present the various applications that Freidinger lactams and their hetero-, fused- and unsaturated analogs have found in the design of conformationally constrained peptidomimetics in different therapeutic areas.

Keywords: Freidinger lactams, dipeptide mimetics, lactam peptidomimetics, conformationally constrained peptide analogs, peptidomimetic design

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Article Details

Year: 2006
Page: [1525 - 1556]
Pages: 32
DOI: 10.2174/092986706777442066
Price: $65

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