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.
Keywords: Diketopiperazine (DKP), microwave (MW)-assisted organic reaction, cyclative cleavage, privileged structure, solid-phase organic synthesis (SPOS), small molecule therapeutic
Combinatorial Chemistry & High Throughput Screening
Title: Solid-Phase and Microwave-Assisted Syntheses of 2,5-Diketopiperazines:Small Molecules with Great Potential
Volume: 10 Issue: 10
Author(s): Jennifer C. O'Neill and Helen E. Blackwell
Affiliation:
Keywords: Diketopiperazine (DKP), microwave (MW)-assisted organic reaction, cyclative cleavage, privileged structure, solid-phase organic synthesis (SPOS), small molecule therapeutic
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.
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Cite this article as:
O'Neill C. Jennifer and Blackwell E. Helen, Solid-Phase and Microwave-Assisted Syntheses of 2,5-Diketopiperazines:Small Molecules with Great Potential, Combinatorial Chemistry & High Throughput Screening 2007; 10 (10) . https://dx.doi.org/10.2174/138620707783220365
DOI https://dx.doi.org/10.2174/138620707783220365 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
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