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New insights into the bacterial RNA polymerase inhibitor CBR703 as a starting point for optimization as an anti-infective agent.
- Source :
-
Antimicrobial agents and chemotherapy [Antimicrob Agents Chemother] 2014 Jul; Vol. 58 (7), pp. 4242-5. Date of Electronic Publication: 2014 May 12. - Publication Year :
- 2014
-
Abstract
- CBR703 was reported to inhibit bacterial RNA polymerase (RNAP) and biofilm formation, considering it to be a good candidate for further optimization. While synthesized derivatives of CBR703 did not result in more-active RNAP inhibitors, we observed promising antibacterial activities. These again correlated with a significant cytotoxicity toward mammalian cells. Furthermore, we suspect the promising effects on biofilm formation to be artifacts. Consequently, this class of compounds can be considered unattractive as antibacterial agents.<br /> (Copyright © 2014, American Society for Microbiology. All Rights Reserved.)
- Subjects :
- Bacillus subtilis drug effects
Bacillus subtilis enzymology
Bacillus subtilis genetics
Cell Line
Escherichia coli enzymology
Escherichia coli genetics
HEK293 Cells
Humans
Microbial Sensitivity Tests
Pseudomonas aeruginosa drug effects
Pseudomonas aeruginosa enzymology
Pseudomonas aeruginosa genetics
RNA, Bacterial biosynthesis
Staphylococcus aureus drug effects
Staphylococcus aureus enzymology
Staphylococcus aureus genetics
Structure-Activity Relationship
Transcription, Genetic drug effects
Amidines pharmacology
Anti-Bacterial Agents pharmacology
DNA-Directed RNA Polymerases antagonists & inhibitors
Enzyme Inhibitors pharmacology
Escherichia coli drug effects
Hydroxylamines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1098-6596
- Volume :
- 58
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- Antimicrobial agents and chemotherapy
- Publication Type :
- Academic Journal
- Accession number :
- 24820077
- Full Text :
- https://doi.org/10.1128/AAC.02600-14