Quorum sensing (QS) plays an essential role in virulence factor production, biofilm formation, and antimicrobial resistance. As a potent QS inhibitor, hordenine can inhibit both QS and biofilm formation in and . In this work, we tested the QS inhibitory potential of 27 hordenine analogs against QS and biofilm formation in and Among the tested analogs, seven (12, 28, 27, 26, 2, 23, and 7) exhibited strong QS inhibitory activity against , five of which (12, 28, 27, 26, and 2) showed better inhibitory activity than hordenine. In addition, seven analogs (28, 12, 23, 7, 26, 2, and 27) exhibited better biofilm inhibition against than hordenine. Four analogs (7, 28, 2, and 12) showed QS inhibitory activity against , two of which (7 and 28) demonstrated better inhibitory activity than hordenine. Furthermore, analog 7 showed similar biofilm inhibition against as hordenine. Structure-activity relationship (SAR) analysis indicated that the inhibitory activities of the analogs were related to four factors, i.e., carbon chain length, presence or absence of an α,β-C[bond, double bond]C bond, amino group with/without lipophilic group, such as methyl group, and hydroxyl group in benzene ring.
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8573111 | PMC |
http://dx.doi.org/10.1016/j.synbio.2021.09.010 | DOI Listing |
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