NDLI: Efficient Construction of Diketopiperazine Macroarrays Through a Cyclative-Cleavage Strategy and Their Evaluation as Luminescence Inhibitors in the Bacterial Symbiont Vibrio fischeri

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Efficient Construction of Diketopiperazine Macroarrays Through a Cyclative-Cleavage Strategy and Their Evaluation as Luminescence Inhibitors in the Bacterial Symbiont Vibrio fischeri

Solution phase synthesis of a diverse isocoumarin library

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Efficient Construction of Diketopiperazine Macroarrays Through a Cyclative-Cleavage Strategy and Their Evaluation as Luminescence Inhibitors in the Bacterial Symbiont Vibrio fischeri

Content Provider	PubMed Central
Author	Campbell, Jennifer Blackwell, Helen E.
Abstract	Diketopiperazines (DKPs) are a well-known class of heterocycles that have 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, often, the discovery of active compounds. We recently identified several DKPs that are capable of inhibiting the luminescence response of the bacterial symbiont Vibrio fischeri, and we sought to further test the scope of this biological activity. Herein, we report the synthesis of DKP macroarrays using a SPOT-synthesis approach based on an Ugi/DeBoc/Cyclize strategy. Neither a spacer nor a linker was required for macroarray construction on cellulose support, and the cyclative cleavage produced high purity DKPs in good yields. Using this protocol, we prepared a library of 400 DKPs on cellulose support and evaluated its members as luminescence inhibitors in V. fischeri. We found six DKPs capable of inhibiting luminescence by greater than 80% at 500 μM. Collectively, this work serves to further highlight the utility of the small molecule macroarray platform for the synthesis and evaluation of focused libraries.
Related Links	http://dx.doi.org/10.1021/cc900115x
Ending Page	1099
Page Count	6
Starting Page	1094
File Format	PDF
ISSN	15204766
e-ISSN	15204774
Journal	Journal of combinatorial chemistry
Issue Number	6
Volume Number	11
Language	English
Publisher Date	2009-11-09
Access Restriction	Open
Subject Keyword	Chemistry(all) Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	Chemistry

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Efficient construction of diketopiperazine macroarrays through a cyclative-cleavage strategy and their evaluation as luminescence inhibitors in the bacterial symbiont Vibrio fischeri.

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Efficient Construction of Diketopiperazine Macroarrays Through a Cyclative-Cleavage Strategy and Their Evaluation as Luminescence Inhibitors in the Bacterial Symbiont Vibrio fischeri

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Efficient construction of diketopiperazine macroarrays through a cyclative-cleavage strategy and their evaluation as luminescence inhibitors in the bacterial symbiont Vibrio fischeri.

The light organ symbiont Vibrio fischeri possesses a homolog of the Vibrio cholerae transmembrane transcriptional activator ToxR.

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Efficient Construction of Diketopiperazine Macroarrays Through a Cyclative-Cleavage Strategy and Their Evaluation as Luminescence Inhibitors in the Bacterial Symbiont Vibrio fischeri