umu.sePublikationer
Ändra sökning
RefereraExporteraLänk till posten
Permanent länk

Direktlänk
Referera
Referensformat
  • apa
  • ieee
  • modern-language-association-8th-edition
  • vancouver
  • Annat format
Fler format
Språk
  • de-DE
  • en-GB
  • en-US
  • fi-FI
  • nn-NO
  • nn-NB
  • sv-SE
  • Annat språk
Fler språk
Utmatningsformat
  • html
  • text
  • asciidoc
  • rtf
Mapping pilicide anti-virulence effect in Escherichia coli, a comprehensive structure-activity study
Umeå universitet, Teknisk-naturvetenskapliga fakulteten, Kemiska institutionen.
Umeå universitet, Teknisk-naturvetenskapliga fakulteten, Kemiska institutionen.
Umeå universitet, Teknisk-naturvetenskapliga fakulteten, Kemiska institutionen. (Umeå Centre for Micobial Research)
Visa övriga samt affilieringar
2012 (Engelska)Ingår i: Bioorganic & Medicinal Chemistry, ISSN 0968-0896, E-ISSN 1464-3391, Vol. 20, nr 9, s. 3128-3142Artikel i tidskrift (Refereegranskat) Published
Abstract [en]

Pilicides prevent pili formation and thereby the development of bacterial biofilms in Escherichia coli. We have performed a comprehensive structure activity relationship (SAR) study of the dihydrothiazolo ring-fused 2-pyridone pilicide central fragment by varying all open positions. Orthogonal projections to latent structures discriminant analysis (OPLS-DA) was used to distinguish active from inactive compounds in which polarity proved to be the most important factor for discrimination. A quantitative SAR (QSAR) partial least squares (PLS) model was calculated on the active compounds for prediction of biofilm inhibition activity. In this model, compounds with high inhibitory activity were generally larger, more lipophilic, more flexible and had a lower HOMO. Overall, this resulted in both highly valuable SAR information and potent inhibitors of type 1 pili dependent biofilm formation. The most potent biofilm inhibitor had an EC(50) of 400nM.

Ort, förlag, år, upplaga, sidor
Elsevier, 2012. Vol. 20, nr 9, s. 3128-3142
Nyckelord [en]
Synechocystis-sp PCC-6803, CAB-like proteins, Alga Chlamydomonas-ReinhardTII, Pigment-Binding Protein, Plant Photosystem-I, State Transitions, Arabidopsis-Thaliana, Antenna Proteins, Gene Family, Inducible Protein
Nationell ämneskategori
Kemi
Identifikatorer
URN: urn:nbn:se:umu:diva-54385DOI: 10.1016/j.bmc.2012.01.048ISI: 000303002100040PubMedID: 22464688OAI: oai:DiVA.org:umu-54385DiVA, id: diva2:523597
Tillgänglig från: 2012-04-25 Skapad: 2012-04-25 Senast uppdaterad: 2018-06-08Bibliografiskt granskad

Open Access i DiVA

Fulltext saknas i DiVA

Övriga länkar

Förlagets fulltextPubMed

Personposter BETA

Chorell, ErikBengtsson, ChristofferEdvinsson, SofieLinusson, AnnaAlmqvist, Fredrik

Sök vidare i DiVA

Av författaren/redaktören
Chorell, ErikBengtsson, ChristofferEdvinsson, SofieLinusson, AnnaAlmqvist, Fredrik
Av organisationen
Kemiska institutionen
I samma tidskrift
Bioorganic & Medicinal Chemistry
Kemi

Sök vidare utanför DiVA

GoogleGoogle Scholar

doi
pubmed
urn-nbn

Altmetricpoäng

doi
pubmed
urn-nbn
Totalt: 347 träffar
RefereraExporteraLänk till posten
Permanent länk

Direktlänk
Referera
Referensformat
  • apa
  • ieee
  • modern-language-association-8th-edition
  • vancouver
  • Annat format
Fler format
Språk
  • de-DE
  • en-GB
  • en-US
  • fi-FI
  • nn-NO
  • nn-NB
  • sv-SE
  • Annat språk
Fler språk
Utmatningsformat
  • html
  • text
  • asciidoc
  • rtf