Structure-Activity Relationships of Phenyl-Furanyl-Rhodanines as Inhibitors of RNA Polymerase with Antibacterial Activity on Biofilms
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- 作者：Philippe Villain-Guillot ; Maxime Gualtieri ; Lionel Bastide ; Franç ; oise Roquet ; Jean Martinez ; Muriel Amblard ; Martine Pugniere ; Jean-Paul Leonetti
- 刊名：Journal of Medicinal Chemistry
- 出版年：2007
- 出版时间：August 23, 2007
- 年：2007
- 卷：50
- 期：17
- 页码：4195 - 4204
- 全文大小：162K
- 年卷期：v.50,no.17(August 23, 2007)
- ISSN：1520-4804
文摘
The dramatic rise of antibiotic-resistant bacteria over the past two decades has stressed the need for completelynovel classes of antibacterial agents. Accordingly, recent advances in the study of prokaryotic transcriptionopen new opportunities for such molecules. This paper reports the structure-activity relationships of aseries of phenyl-furanyl-rhodanines (PFRs) as antibacterial inhibitors of RNA polymerase (RNAP). Themolecules have been evaluated for their ability to inhibit transcription and affect growth of bacteria livingin suspension or in a biofilm and for their propensity to interact with serum albumin, a critical parameterfor antibacterial drug discovery. The most active of these molecules inhibit Escherichia coli RNAPtranscription at concentrations of 
10 
M and have promising activities against various Gram-positivepathogens including Staphylococcus epidermidis biofilms, a major cause of nosocomial infection.
10 M and have promising activities against various Gram-positivepathogens including Staphylococcus epidermidis biofilms, a major cause of nosocomial infection.