Solid-phase and microwave-assisted syntheses of 2,5-diketopiperazines: small molecules with great potential.
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.
O'Neill
Jennifer C
JC
Department of Chemistry, University of Wisconsin-Madison, 1101 University Avenue, Madison, WI 53706, USA.
Blackwell
Helen E
HE
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis*; D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D054659:Diketopiperazines / Q000138:chemical synthesis*; D008872:Microwaves; D008956:Models, Chemical
D000900:Anti-Bacterial Agents; D054659:Diketopiperazines