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Structure-activity relationships of phenyl-furanyl-rhodanines as inhibitors of RNA polymerase with antibacterial activity on biofilms
- Source :
- Journal of Medicinal Chemistry, Journal of Medicinal Chemistry, American Chemical Society, 2007, 50 (17), pp.4195-204. ⟨10.1021/jm0703183⟩
- Publication Year :
- 2007
- Publisher :
- HAL CCSD, 2007.
-
Abstract
- The dramatic rise of antibiotic-resistant bacteria over the past two decades has stressed the need for completely novel classes of antibacterial agents. Accordingly, recent advances in the study of prokaryotic transcription open new opportunities for such molecules. This paper reports the structure-activity relationships of a series of phenyl-furanyl-rhodanines (PFRs) as antibacterial inhibitors of RNA polymerase (RNAP). The molecules have been evaluated for their ability to inhibit transcription and affect growth of bacteria living in suspension or in a biofilm and for their propensity to interact with serum albumin, a critical parameter for antibacterial drug discovery. The most active of these molecules inhibit Escherichia coli RNAP transcription at concentrations of/=10 microM and have promising activities against various Gram-positive pathogens including Staphylococcus epidermidis biofilms, a major cause of nosocomial infection.
- Subjects :
- Rhodanine
MESH: Staphylococcus epidermidis
MESH: Cricetinae
CHO Cells
Microbial Sensitivity Tests
MESH: Biofilms
[SDV.BC]Life Sciences [q-bio]/Cellular Biology
Gram-Positive Bacteria
010402 general chemistry
01 natural sciences
MESH: Gram-Positive Bacteria
Structure-Activity Relationship
chemistry.chemical_compound
Cricetulus
MESH: Structure-Activity Relationship
MESH: Cricetulus
Staphylococcus epidermidis
Bacterial transcription
Transcription (biology)
MESH: CHO Cells
Cricetinae
RNA polymerase
MESH: Anti-Bacterial Agents
Drug Discovery
Animals
MESH: Animals
Furans
Antibacterial agent
MESH: Microbial Sensitivity Tests
biology
MESH: Rhodanine
010405 organic chemistry
Chemistry
MESH: Furans
Biofilm
DNA-Directed RNA Polymerases
biology.organism_classification
Anti-Bacterial Agents
3. Good health
0104 chemical sciences
MESH: DNA-Directed RNA Polymerases
Biochemistry
Biofilms
Molecular Medicine
Antibacterial activity
Bacteria
Subjects
Details
- Language :
- English
- ISSN :
- 00222623 and 15204804
- Database :
- OpenAIRE
- Journal :
- Journal of Medicinal Chemistry, Journal of Medicinal Chemistry, American Chemical Society, 2007, 50 (17), pp.4195-204. ⟨10.1021/jm0703183⟩
- Accession number :
- edsair.doi.dedup.....4fe0c398c0073f13f0bb6660b79e8775