2.50
Hdl Handle:
http://hdl.handle.net/10033/322701
Title:
Benzamidobenzoic acids as potent PqsD inhibitors for the treatment of Pseudomonas aeruginosa infections.
Authors:
Hinsberger, Stefan; de Jong, Johannes C; Groh, Matthias; Haupenthal, Jörg; Hartmann, Rolf W
Abstract:
Targeting PqsD is a promising novel approach to disrupt bacterial cell-to-cell-communication in Pseudomonas aeruginosa. In search of selective PqsD inhibitors, two series of benzamidobenzoic acids - one published as RNAP inhibitors and the other as PqsD inhibitors - were investigated for inhibitory activity toward the respective other enzyme. Additionally, novel derivatives were synthesized and biologically evaluated. By this means, the structural features needed for benzamidobenzoic acids to be potent and, most notably, selective PqsD inhibitors were identified. The most interesting compound of this study was the 3-Cl substituted compound 5 which strongly inhibits PqsD (IC₅₀ 6.2 μM) while exhibiting no inhibition of RNAP.
Citation:
Benzamidobenzoic acids as potent PqsD inhibitors for the treatment of Pseudomonas aeruginosa infections. 2014, 76:343-51 Eur J Med Chem
Journal:
European journal of medicinal chemistry
Issue Date:
9-Apr-2014
URI:
http://hdl.handle.net/10033/322701
DOI:
10.1016/j.ejmech.2014.02.014
PubMed ID:
24589489
Type:
Article
Language:
en
ISSN:
1768-3254
Appears in Collections:
publications of the department drug design and optimization (HIPS]DDOP)

Full metadata record

DC FieldValue Language
dc.contributor.authorHinsberger, Stefanen
dc.contributor.authorde Jong, Johannes Cen
dc.contributor.authorGroh, Matthiasen
dc.contributor.authorHaupenthal, Jörgen
dc.contributor.authorHartmann, Rolf Wen
dc.date.accessioned2014-07-09T14:37:21Z-
dc.date.available2014-07-09T14:37:21Z-
dc.date.issued2014-04-09-
dc.identifier.citationBenzamidobenzoic acids as potent PqsD inhibitors for the treatment of Pseudomonas aeruginosa infections. 2014, 76:343-51 Eur J Med Chemen
dc.identifier.issn1768-3254-
dc.identifier.pmid24589489-
dc.identifier.doi10.1016/j.ejmech.2014.02.014-
dc.identifier.urihttp://hdl.handle.net/10033/322701-
dc.description.abstractTargeting PqsD is a promising novel approach to disrupt bacterial cell-to-cell-communication in Pseudomonas aeruginosa. In search of selective PqsD inhibitors, two series of benzamidobenzoic acids - one published as RNAP inhibitors and the other as PqsD inhibitors - were investigated for inhibitory activity toward the respective other enzyme. Additionally, novel derivatives were synthesized and biologically evaluated. By this means, the structural features needed for benzamidobenzoic acids to be potent and, most notably, selective PqsD inhibitors were identified. The most interesting compound of this study was the 3-Cl substituted compound 5 which strongly inhibits PqsD (IC₅₀ 6.2 μM) while exhibiting no inhibition of RNAP.en
dc.language.isoenen
dc.rightsArchived with thanks to European journal of medicinal chemistryen
dc.titleBenzamidobenzoic acids as potent PqsD inhibitors for the treatment of Pseudomonas aeruginosa infections.en
dc.typeArticleen
dc.identifier.journalEuropean journal of medicinal chemistryen

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