Furanyl-rhodanines are unattractive drug candidates for development as inhibitors of bacterial RNA polymerase

Antimicrobial Agents and Chemotherapy

Volumn 54, Issue 10, 2010, Pages 4506-4509

  Mariner, Katherine R ^a   Trowbridge, Rachel ^a   Agarwal, Anil K ^a   Miller, Keith ^a,b   O'Neill, Alex J ^a   Fishwick, Colin W G ^a   Chopra, Ian ^a  

^a UNIVERSITY OF LEEDS   (United Kingdom)

^b SHEFFIELD HALLAM UNIVERSITY   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

CHYMOTRYPSIN; CORALLOPYRONIN A; MALATE DEHYDROGENASE; RHODANINE; RIFAMPICIN; RIFAMYCIN; RNA POLYMERASE; UNCLASSIFIED DRUG;

ANTIBACTERIAL ACTIVITY; ARTICLE; ASSAY; BIOSENSOR; DNA SYNTHESIS; MACROMOLECULE; MEMBRANE DAMAGE; MINIMUM INHIBITORY CONCENTRATION; NONHUMAN; PRIORITY JOURNAL;

ANTI-BACTERIAL AGENTS; BACTERIAL PROTEINS; CELL MEMBRANE; CHYMOTRYPSIN; DNA-DIRECTED RNA POLYMERASES; ENZYME INHIBITORS; MALATE DEHYDROGENASE; RHODANINE;

EID: 77957368559     PISSN: 00664804     EISSN: 10986596     Source Type: Journal    
DOI: 10.1128/AAC.00753-10     Document Type: Article

References (16)

1. Agarwal, A. K., A. P. Johnson, and C. W. G. Fishwick. 2008. Synthesis of de novo designed small-molecule inhibitors of bacterial RNA polymerase. Tetrahedron 64:10049-10054.
2. Chopra, I. 2007. Bacterial RNA polymerase: a promising target for the discovery of new antimicrobial agents. Curr. Opin. Invest. Drugs 8:600-607.
3. Dixon, R., and I. Chopra. 1986. Leakage of periplasmic proteins from Escherichia coli mediated by the polymyxin analogue, polymyxin B nonapeptide. Antimicrob. Agents Chemother. 29:781-788.
4. Grant, E. B., D. Guiadeen, E. Z. Baum, B. D. Foleno, H. Jin, D. A. Montenegro, E. A. Nelson, K. Bush, and D. J. Hlasta. 2000. The synthesis and SAR of rhodanines as novel class C β-lactamase inhibitors. Bioorg. Med. Chem. Lett. 10:2179-2182.
5. Hobbs, J. K., K. Miller, A. J. O'Neill, and I. Chopra. 2008. Consequences of daptomycin-mediated membrane damage in Staphylococcus aureus. J. Antimicrob. Chemother. 62:1003-1008.
6. B modulates virulence determinant expression and stress resistance: characterization of a functional rsbU strain derived from Staphylococcus aureus 8325-4. J. Bacteriol. 184:5457-5467.
7. Irschik, H., R. Jansen, G. Hofle, K. Gerth, and H. Reichenbach. 1985. The corallopyronins, new inhibitors of bacterial RNA synthesis from myxobacteria. J. Antibiot. 38:144-152. (Pubitemid 15131944)
8. Mariani, R., and S. J. Maffioli. 2009. Bacterial RNA polymerase inhibitors: an organized overview of their structure, derivatives, biological activity and current clinical development status. Curr. Med. Chem. 16:430-454.
9. O'Neill, A. J., J. Bostock, A. Morais-Moita, and I. Chopra. 2002. Antimicrobial activity and mechanisms of resistance to cephalosporin P1, an antibiotic related to fusidic acid. J. Antimicrob. Chemother. 50:839-848.
10. O'Neill, A., B. Oliva, C. Storey, A. Hoyle, C. Fishwick, and I. Chopra. 2000. RNA polymerase inhibitors with activity against rifampin-resistant mutants of Staphylococcus aureus. Antimicrob. Agents Chemother. 44:3163-3166.
11. Report of the Working Party on Antibiotic Sensitivity Testing of the British Society for Antimicrobial Chemotherapy. 1991. A guide to sensitivity testing. J. Antimicrob. Chemother. 27(Suppl. D):1-50.
12. Seidler, J., S. L. McGovern, T. N. Doman, and B. K. Shoichet. 2003. Identification and prediction of promiscuous aggregating inhibitors among known drugs. J. Med. Chem. 46:4477-4486.
13. Urban, A., S. Eckermann, B. Fast, S. Metzger, M. Gehling, K. Zielgelbauer, H. Rubsamen, and C. Freiberg. 2007. Novel whole-cell antibiotic biosensors for compound discovery. Appl. Environ. Microbiol. 73:6436-6443.
14. Villain-Guillot, P., L. Bastide, M. Gualtieri, and J.-P. Leonetti. 2007. Progress in targeting bacterial transcription. Drug Discov. Today 12:200-208.
15. Villain-Guillot, P., M. Gualtieri, L. Bastide, F. J. Roquet, J. Martinez, M. Amblard, M. Pugniere, and J.-P. Leonetti. 2007. Structure-activity relationships of phenyl-furanyl-rhodanines as inhibitors of RNA polymerase with antibacterial activity on biofilms. J. Med. Chem. 50:4195-4204.
16. Zervosen, A., L. Wei-Ping, Z. Chen, R. E. White, T. M. Demuth, and J. M. Frere. 2004. Interactions between penicillin-binding proteins (PBPs) and two novel classes of PBP inhibitors, arylalkylidene rhodanines and arylalkylidene iminothiazolidin-4-ones. Antimicrob. Agents Chemother. 48:961-969.