Benzamidobenzoic acids as potent PqsD inhibitors for the treatment of Pseudomonas aeruginosa infections.

Hinsberger, Stefan; de Jong, Johannes C; Groh, Matthias; Haupenthal, Jörg; Hartmann, Rolf W

dc.contributor.author	Hinsberger, Stefan
dc.contributor.author	de Jong, Johannes C
dc.contributor.author	Groh, Matthias
dc.contributor.author	Haupenthal, Jörg
dc.contributor.author	Hartmann, Rolf W
dc.date.accessioned	2014-07-09T14:37:21Z
dc.date.available	2014-07-09T14:37:21Z
dc.date.issued	2014-04-09
dc.identifier.citation	Benzamidobenzoic acids as potent PqsD inhibitors for the treatment of Pseudomonas aeruginosa infections. 2014, 76:343-51 Eur J Med Chem	en
dc.identifier.issn	1768-3254
dc.identifier.pmid	24589489
dc.identifier.doi	10.1016/j.ejmech.2014.02.014
dc.identifier.uri	http://hdl.handle.net/10033/322701
dc.description.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.
dc.language.iso	en	en
dc.rights	Archived with thanks to European journal of medicinal chemistry	en
dc.title	Benzamidobenzoic acids as potent PqsD inhibitors for the treatment of Pseudomonas aeruginosa infections.	en
dc.type	Article	en
dc.identifier.journal	European journal of medicinal chemistry	en
refterms.dateFOA	2018-06-12T20:01:54Z
html.description.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.