Identification of novel phenylalanine derivatives bearing a hydroxamic acid moiety as potent quorum sensing inhibitors.

ABSTRACT: Phenylalanine derivatives are a well-known small moiety responsible for controlling the virulence factors of several bacteria. Herein, for the first time, we report novel structures of phenylalanine derivatives bearing a hydroxamic acid moiety which were designed, synthesized, and evaluated for use as quorum sensing inhibitors. Biological results reveal that six compounds showed good quorum sensing inhibitors properties with an IC₅₀ ranging from 7.12 ± 2.11 μM-92.34 ± 2.09 μM (4NPO, a reference compound, IC₅₀ = 29.13 ± 0.88 μM). In addition, three out of the six compounds (4a, 4c, 4h) showed strong anti-biofilm formation and CviR inhibitory activity when compared to that of 4NPO. These biological data were also confirmed by computational studies. In this series

SUBMITTER: Tung TT 

PROVIDER: S-EPMC11042162 | biostudies-literature | 2024 Apr

REPOSITORIES: biostudies-literature