@article{2d23822044fa4e929cec972c05e6a814,
title = "Cadiolide analogues and their precursors as new inhibitors of bacterial quorum sensing and biofilm formation",
abstract = "Bacterial quorum sensing (QS) and biofilm formation are promising targets for developing new therapies to treat chronic infections. Herein, we report the stereoselective synthesis of 18 new analogs of natural cadiolides. Among the new compounds, substances 8b, 8f, 8i, 9a, 9b and 9e completely inhibited the biofilm formation of Escherichia coli RP347 in vitro. In addition, compound 8b interfered acyl-homoserine lactone (AHL) mediated QS, while 9e interrupted the QS via autoinducer-2 (AI-2). Biological assays also revealed that synthetic intermediates alkynones are potent inhibitors of AI-2 and AHL-mediated QS. These results indicate that cadiolides and alkynones are good candidates for further structural modification for a new generation of more potent antimicrobial agents.",
keywords = "Alkynone, Anti-biofilm agents, Cadiolides, Quorum sensing",
author = "Moreira, {Thais A.} and Antol{\'i}nez, {Isabel V.} and Valen{\c c}a, {Wagner O.} and Sweta Roy and Barbosa, {Luiz C.A.} and Dacheng Ren",
note = "Funding Information: We are grateful to the following Brazilian agencies: Conselho Nacional de Desenvolvimento Cient{\'i}f{\'i}co e Tecnol{\'o}gico (CNPq, grant 304445/2017-7) and for research fellowships (LCAB, MHA, and RD); Funda{\c c}{\~a}o de Amparo {\`a} Pesquisa de Minas Gerais (FAPEMIG grant APQ1557-15) for financial support; Coordena{\c c}{\~a}o de Aperfei{\c c}oamento de Pessoal de N{\'i}vel Superior ( CAPES , Grant 001) for a research fellowship (T.A.M, I.V.A. and W.A.V.). Related work in the Ren group was supported by the Stevenson endowment funds. Funding Information: We are grateful to the following Brazilian agencies: Conselho Nacional de Desenvolvimento Cient?f?co e Tecnol?gico (CNPq, grant 304445/2017-7) and for research fellowships (LCAB, MHA, and RD); Funda??o de Amparo ? Pesquisa de Minas Gerais (FAPEMIG grant APQ1557-15) for financial support; Coordena??o de Aperfei?oamento de Pessoal de N?vel Superior (CAPES, Grant 001) for a research fellowship (T.A.M, I.V.A. and W.A.V.). Related work in the Ren group was supported by the Stevenson endowment funds. Publisher Copyright: {\textcopyright} 2021 Elsevier Ltd",
year = "2022",
month = feb,
day = "1",
doi = "10.1016/j.bmcl.2021.128498",
language = "English (US)",
volume = "57",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier",
}