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Combinatorial Chemistry & High Throughput Screening


ISSN (Print): 1386-2073
ISSN (Online): 1875-5402

Solid-Phase and Microwave-Assisted Syntheses of 2,5-Diketopiperazines:Small Molecules with Great Potential

Author(s): Jennifer C. O'Neill and Helen E. Blackwell

Volume 10 , Issue 10 , 2007

Page: [857 - 876] Pages: 20

DOI: 10.2174/138620707783220365

Price: $65


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

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