Abstract:
:In an attempt to counteract bacterial pathogenicity, a set of novel imidazolidine-2,4-dione and 2-thioxoimidazolidin-4-one derivatives was synthesized and evaluated as inhibitors of bacterial virulence. The new compounds were characterized and screened for their effects on the expression of virulence factors of Pseudomonas aeruginosa, including protease, hemolysin, and pyocyanin. Imidazolidine-2,4-diones 4c, 4j, and 12a showed complete inhibition of the protease enzyme, and they almost completely inhibited the production of hemolysin at 1/4 MIC (1/4 minimum inhibitory concentration; 1, 0.5, and 0.5 mg/ml, respectively). 2-Thioxoimidazolidin-4-one derivative 7a exhibited the best inhibitory activity (96.4%) against pyocyanin production at 1 mg/ml (1/4 MIC). A docking study was preformed to explore the potential binding interactions with quorum-sensing receptors (LasR and RhlR), which are responsible for the expression of virulence genes.
journal_name
Arch Pharm (Weinheim)journal_title
Archiv der Pharmazieauthors
Mohamed B,Abdel-Samii ZK,Abdel-Aal EH,Abbas HA,Shaldam MA,Ghanim AMdoi
10.1002/ardp.201900352subject
Has Abstractpub_date
2020-05-01 00:00:00pages
e1900352issue
5eissn
0365-6233issn
1521-4184journal_volume
353pub_type
杂志文章abstract::Twelve ethoxycarbonyl or phenylsulfonyl derivatives as prodrugs of hydroxylamine or phenylhydroxylamine were prepared and tested for antiplatelet (in vitro, Born test) antithrombotic (in vivo thrombosis model), and antihypertensive (in vivo, SHR rats) effects. In the Born test N,N-bisphenylsulfonylhydroxylamine (10) w...
journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
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pub_type: 杂志文章
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
doi:
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
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更新日期:1997-04-01 00:00:00
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
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journal_title:Archiv der Pharmazie
pub_type: 杂志文章
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更新日期:1995-10-01 00:00:00