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Title: Dihydropyrrolones as bacterial quorum sensing inhibitors
Authors: Almohaywi, Basmah
Yu, Tsz Tin
Iskander, George
Chan, Daniel S. H.
Ho, Kitty K. K.
Rice, Scott A.
Black, David StC.
Griffith, Renate
Kumar, Naresh
Keywords: Science::Biological sciences
Issue Date: 2019
Source: Almohaywi, B., Yu, T. T., Iskander, G., Chan, D. S. H., Ho, K. K. K., Rice, S. A., . . . Kumar N. (2019). Dihydropyrrolones as bacterial quorum sensing inhibitors. Bioorganic and Medicinal Chemistry Letters, 29(9), 1054-1059. doi:10.1016/j.bmcl.2019.03.004
Journal: Bioorganic and Medicinal Chemistry Letters
Abstract: Bacteria regulate their pathogenicity and biofilm formation through quorum sensing (QS), which is an intercellular communication system mediated by the binding of signaling molecules to QS receptors such as LasR. In this study, a range of dihydropyrrolone (DHP) analogues were synthesized via the lactone-lactam conversion of lactone intermediates. The synthesized compounds were tested for their ability to inhibit QS, biofilm formation and bacterial growth of Pseudomonas aeruginosa. The compounds were also docked into a LasR crystal structure to rationalize the observed structure-activity relationships. The most active compound identified in this study was compound 9i, which showed 63.1% QS inhibition of at 31.25 µM and 60% biofilm reduction at 250 µM with only moderate toxicity towards bacterial cell growth.
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2019.03.004
Rights: © 2019 Elsevier Ltd. All rights reserved.
Fulltext Permission: none
Fulltext Availability: No Fulltext
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