2,5-二酮哌嗪的固相合成与微波辅助合成：具有巨大潜力的小分子
Solid-phase and microwave-assisted syntheses of 2,5-diketopiperazines: small molecules with great potential.
作者信息
O'Neill Jennifer C, Blackwell Helen E
机构信息
Department of Chemistry, University of Wisconsin-Madison, 1101 University Avenue, Madison, WI 53706, USA.
出版信息
Comb Chem High Throughput Screen. 2007 Dec;10(10):857-76. doi: 10.2174/138620707783220365.
Abstract
Diketopiperazines (DKPs) are a well-known class of heterocycles that have recently emerged as a promising biologically active scaffold. Solid-phase organic synthesis has become an important tool in the combinatorial exploration of these privileged structures, expediting the synthesis and, therefore, the discovery of active compounds. To date, certain DKPs have shown potent activities against a range of diseases and biological phenomena, including bacterial infections, various cancers, asthma, infertility, premature labor, and HIV. Recent applications of solid-phase DKP synthesis, with a particular focus on cyclative cleavage and microwave-assisted reactions, are highlighted herein.
摘要
二酮哌嗪（DKPs）是一类著名的杂环化合物，最近已成为一种有前景的生物活性骨架。固相有机合成已成为对这些特殊结构进行组合探索的重要工具，加快了活性化合物的合成及发现。迄今为止，某些二酮哌嗪已显示出对一系列疾病和生物现象具有强效活性，包括细菌感染、各种癌症、哮喘、不孕症、早产和艾滋病毒。本文重点介绍了固相二酮哌嗪合成的最新应用，尤其关注环化裂解和微波辅助反应。
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