ArticleJournal of combinatorial chemistry
Efficient construction of diketopiperazine macroarrays through a cyclative-cleavage strategy and their evaluation as luminescence inhibitors in the bacterial symbiont Vibrio fischeri.
Article in Journal of combinatorial chemistry. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed, 30 citations in OpenAlex.
- Quorum quenching activity of endophyticCurrent research in microbial sciences · 2024Article
- Bacterial diketopiperazines stimulate diatom growth and lipid accumulation.Plant physiology · 2021Article
- Isocyanide Multicomponent Reactions on Solid Phase: State of the Art and Future Application.International journal of molecular sciences · 2020Review
- Chemical methods to interrogate bacterial quorum sensing pathways.Organic & biomolecular chemistry · 2012Article
- Expedient construction of small molecule macroarrays via sequential palladium- and copper-mediated reactions and their ex situ biological testing.Chemical science · 2012Article
- Diversity-oriented synthesis of macrocyclic peptidomimetics.Proceedings of the National Academy of Sciences of the United States of America · 2011Article
- Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2009.Journal of combinatorial chemistry · 2010Review
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
Diketopiperazines (DKPs) are a well-known class of heterocycles that have emerged as promising biologically active scaffolds. 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 at least 80% at 500 muM. Collectively, this work serves to further highlight the utility of the small molecule macroarray platform for the synthesis and evaluation of focused libraries.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.