Matches in SemOpenAlex for { <https://semopenalex.org/work/W4309344343> ?p ?o ?g. }
- W4309344343 endingPage "106266" @default.
- W4309344343 startingPage "106266" @default.
- W4309344343 abstract "The antibiotic crisis is associated with the appearance of multidrug resistant (MDR) pathogens, which has caused severe bacterial infections and imposed a huge burden on modern society. Therefore, there is an urgent need to develop new antibacterial drugs with novel mechanism of action. Here we designed and synthesized three series of benzoxazolone, oxazolopyridinone and 3-(2-hydroxyphenyl)hydantoin derivatives and evaluated their activity as novel quorum sensing (QS) inhibitors. We found that benzoxazolone and oxazolopyridinone derivatives had promising QS inhibitory activity in the minimum inhibitory concentration, pyocyanin and rhamnolipid inhibition assays. In particular, A10 and B20 at 256 μg/mL not only suppressed pyocyanin production regulated by QS in P. aeruginosa PAO1 by 36.55% and 46.90%, respectively, but also showed the strongest rhamnolipid inhibitory activity with the IC50 values of 66.35 and 56.75 µg/mL, respectively. Further studies demonstrated that B20 at 64 μg/mL inhibited biofilm formation in P. aeruginosa PAO1 by 40%, and weakened its swarming motility. More importantly, the bacterial mortality of B20 combined with ciprofloxacin and clarithromycin against P. aeruginosa were 48.27% and 49.79%, respectively, while ciprofloxacin and clarithromycin had only 16.99% and 29.11% of bacterial mortality against P. aeruginosa when used alone. Mechanistic studies indicated that B20 directly inhibited the QS pathway based on the GFP reporter strain assay. Overall, this compound with oxazolopyridinone core could serve as an antibacterial lead of QS inhibitor for further evaluation of its drug-likeness." @default.
- W4309344343 created "2022-11-26" @default.
- W4309344343 creator A5001839326 @default.
- W4309344343 creator A5010643835 @default.
- W4309344343 creator A5024700160 @default.
- W4309344343 creator A5027176913 @default.
- W4309344343 creator A5043542554 @default.
- W4309344343 creator A5052500354 @default.
- W4309344343 creator A5058333204 @default.
- W4309344343 creator A5069692306 @default.
- W4309344343 creator A5070169405 @default.
- W4309344343 date "2023-01-01" @default.
- W4309344343 modified "2023-10-17" @default.
- W4309344343 title "Design, synthesis and evaluation of oxazolopyridinone derivatives as quorum sensing inhibitors" @default.
- W4309344343 cites W17631051 @default.
- W4309344343 cites W1978436399 @default.
- W4309344343 cites W1979455969 @default.
- W4309344343 cites W1990607736 @default.
- W4309344343 cites W2048843475 @default.
- W4309344343 cites W2061520106 @default.
- W4309344343 cites W2068316858 @default.
- W4309344343 cites W2095500933 @default.
- W4309344343 cites W2098549678 @default.
- W4309344343 cites W2135782606 @default.
- W4309344343 cites W2138139413 @default.
- W4309344343 cites W2146292204 @default.
- W4309344343 cites W2154447238 @default.
- W4309344343 cites W2475881350 @default.
- W4309344343 cites W2845957415 @default.
- W4309344343 cites W2912621545 @default.
- W4309344343 cites W2951980590 @default.
- W4309344343 cites W2974879367 @default.
- W4309344343 cites W3011000950 @default.
- W4309344343 cites W3081918250 @default.
- W4309344343 cites W3093180567 @default.
- W4309344343 cites W3136759802 @default.
- W4309344343 cites W3159163153 @default.
- W4309344343 cites W3183345530 @default.
- W4309344343 cites W4200349186 @default.
- W4309344343 cites W4200612589 @default.
- W4309344343 doi "https://doi.org/10.1016/j.bioorg.2022.106266" @default.
- W4309344343 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/36399865" @default.
- W4309344343 hasPublicationYear "2023" @default.
- W4309344343 type Work @default.
- W4309344343 citedByCount "1" @default.
- W4309344343 crossrefType "journal-article" @default.
- W4309344343 hasAuthorship W4309344343A5001839326 @default.
- W4309344343 hasAuthorship W4309344343A5010643835 @default.
- W4309344343 hasAuthorship W4309344343A5024700160 @default.
- W4309344343 hasAuthorship W4309344343A5027176913 @default.
- W4309344343 hasAuthorship W4309344343A5043542554 @default.
- W4309344343 hasAuthorship W4309344343A5052500354 @default.
- W4309344343 hasAuthorship W4309344343A5058333204 @default.
- W4309344343 hasAuthorship W4309344343A5069692306 @default.
- W4309344343 hasAuthorship W4309344343A5070169405 @default.
- W4309344343 hasConcept C104317684 @default.
- W4309344343 hasConcept C118687296 @default.
- W4309344343 hasConcept C133936738 @default.
- W4309344343 hasConcept C176947019 @default.
- W4309344343 hasConcept C185592680 @default.
- W4309344343 hasConcept C186380895 @default.
- W4309344343 hasConcept C202751555 @default.
- W4309344343 hasConcept C2776962512 @default.
- W4309344343 hasConcept C2777637488 @default.
- W4309344343 hasConcept C2777752497 @default.
- W4309344343 hasConcept C2778512257 @default.
- W4309344343 hasConcept C2778549369 @default.
- W4309344343 hasConcept C2778746504 @default.
- W4309344343 hasConcept C2780104969 @default.
- W4309344343 hasConcept C2781427627 @default.
- W4309344343 hasConcept C501593827 @default.
- W4309344343 hasConcept C523546767 @default.
- W4309344343 hasConcept C54355233 @default.
- W4309344343 hasConcept C55493867 @default.
- W4309344343 hasConcept C58123911 @default.
- W4309344343 hasConcept C60987743 @default.
- W4309344343 hasConcept C86803240 @default.
- W4309344343 hasConcept C89423630 @default.
- W4309344343 hasConcept C98274493 @default.
- W4309344343 hasConceptScore W4309344343C104317684 @default.
- W4309344343 hasConceptScore W4309344343C118687296 @default.
- W4309344343 hasConceptScore W4309344343C133936738 @default.
- W4309344343 hasConceptScore W4309344343C176947019 @default.
- W4309344343 hasConceptScore W4309344343C185592680 @default.
- W4309344343 hasConceptScore W4309344343C186380895 @default.
- W4309344343 hasConceptScore W4309344343C202751555 @default.
- W4309344343 hasConceptScore W4309344343C2776962512 @default.
- W4309344343 hasConceptScore W4309344343C2777637488 @default.
- W4309344343 hasConceptScore W4309344343C2777752497 @default.
- W4309344343 hasConceptScore W4309344343C2778512257 @default.
- W4309344343 hasConceptScore W4309344343C2778549369 @default.
- W4309344343 hasConceptScore W4309344343C2778746504 @default.
- W4309344343 hasConceptScore W4309344343C2780104969 @default.
- W4309344343 hasConceptScore W4309344343C2781427627 @default.
- W4309344343 hasConceptScore W4309344343C501593827 @default.
- W4309344343 hasConceptScore W4309344343C523546767 @default.
- W4309344343 hasConceptScore W4309344343C54355233 @default.
- W4309344343 hasConceptScore W4309344343C55493867 @default.