Application of a novel design paradigm to generate general nonpeptide combinatorial scaffolds mimicking beta turns: Synthesis of Ligands for somatostatin receptors

被引：23

作者：

Chianelli, D

Kim, YC

Lvovskiy, D

Webb, TR

机构：

[1] ChemBridge Res Labs LLC, San Diego, CA 92127 USA

[2] ChemBridge Corp, San Diego, CA 92127 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2003年 / 11卷 / 23期

关键词：

D O I：

10.1016/j.bmc.2003.08.022

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Nonpeptide compounds that mimic bioactive peptides are desirable for a number of clinical indications. We report a new practical method for the design of scaffolds exhibiting drug-like properties that are suitable for the display of peptide pharmacophores. The synthesis of various synthons of 7'-hydroxy-2',3'-dihydro-1'H,2H,5H-spiro[imidazolidine-4,4'-quinoline]-2,5-dione (1) and methods for the introduction of several mimics of amino acid side-chains are described. This method is exemplified by derivatives that show agonist activity for the somatostatin type 2 receptor. (C) 2003 Elsevier Ltd. All rights reserved.

引用

收藏

页码：5059 / 5068

页数：10

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