Solid-phase synthesis of hydroxyproline-based cyclic hexapeptides

被引：7

作者：

Basso, A ^{[1
]}

Ernst, B ^{[1
]}

机构：

[1] Univ Basel, Pharmactr, Inst Mol Pharm, CH-4056 Basel, Switzerland

来源：

TETRAHEDRON LETTERS | 2001年 / 42卷 / 38期

关键词：

solid-phase synthesis; cyclic peptides; Selectin-antagonists; DHP-linker;

D O I：

10.1016/S0040-4039(01)01368-5

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Cyclic peptides are excellent tools to investigate the functional and spatial requirements for ligands to bind to a given target. In this paper we report the synthesis of a library of cyclic hexapeptides, designed to be Selectin antagonists. Based on molecular modelling calculations, these peptides contain a hydroxyproline building block that serves also as the point of attachment to the solid phase. A modified THP linker has been prepared to bind the hydroxy group of this amino acid to aminomethyl SynPhase(TM) Lanterns. Amino acids of the D- and L-series are used and their influence onto the cyclisation step is also investigated. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：6687 / 6690

页数：4

共 24 条

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[2] Solid-phase synthesis and structural characterization of highly substituted hydroxyproline-based 2,5-diketopiperazines [J].