The DOI matches its Crossref record; 92 of the 92 references it cites were found in a registry or an index.
The oxazolidinones: past, present, and future
Abstract
The success of linezolid stimulated significant efforts to discover new agents in the oxazolidinone class. Over a dozen oxazolidinones have reached the clinic, but many were discontinued due to lack of differentiated potency, inadequate pharmacokinetics, and safety risks that included myelosuppression. Four oxazolidinones are currently undergoing clinical evaluation. The Trius Therapeutics compound tedizolid phosphate (formerly known as torezolid phosphate, TR‐701, DA‐7218), the most advanced, is in phase 3 clinical trials for acute bacterial skin and skin structure infections. Rib‐X completed two phase 2 studies for radezolid (Rx‐01_667, RX‐1741) in uncomplicated skin and skin structure infections and community‐acquired pneumonia. Pfizer and AstraZeneca have each identified antitubercular compounds that have completed phase 1 studies: sutezolid (PNU‐100480, PF‐02341272) and AZD5847 (AZD2563), respectively. The oxazolidinones share a relatively low frequency of resistance largely due to the requirement of mutations in 23S ribosomal RNA genes. However, maintaining potency against strains carrying the mobile cfr gene poses a challenge for the oxazolidinone class, as well as other 50S ribosome inhibitors that target the peptidyl transferase center.
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Cites
rrndb: the Ribosomal RNA Operon Copy Number Database
Klappenbach, J. A. (2001) · Nucleic Acids Research · doi:10.1093/nar/29.1.181 · Cited by 1,081
Schlünzen, F., Zarivach, R., Harms, J., Bashan, A., Tocilj, A., Albrecht, R., Yonath, A., & Franceschi, F. (2001) · Nature · doi:10.1038/35101544 · Cited by 1,059
Linezolid resistance in a clinical isolate of Staphylococcus aureus
Tsiodras, S., Gold, H. S., Sakoulas, G., Eliopoulos, G. M., Wennersten, C., Venkataraman, L., Moellering, R. C., & Ferraro, M. J. (2001) · The Lancet · doi:10.1016/s0140-6736(01)05410-1 · Cited by 1,033
Long, K. S., Poehlsgaard, J., Kehrenberg, C., Schwarz, S., & Vester, B. (2006) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.00131-06 · Cited by 708
Brickner, S. J., Hutchinson, D. K., Barbachyn, M. R., Manninen, P. R., Ulanowicz, D. A., Garmon, S. A., Grega, K. C., Hendges, S. K., Toops, D. S., Ford, C. W., et al. (1996) · Journal of Medicinal Chemistry · doi:10.1021/jm9509556 · Cited by 582
Self-citationOxazolidinone Structure–Activity Relationships Leading to Linezolid
Barbachyn, M. R., & Ford, C. W. (2003) · Angewandte Chemie International Edition · doi:10.1002/anie.200200528 · Cited by 553
Self-citationInfections due to vancomycin-resistant Enterococcus faecium resistant to linezolid
Gonzales, R. D., Schreckenberger, P. C., Graham, M. B., Kelkar, S., DenBesten, K., & Quinn, J. P. (2001) · The Lancet · doi:10.1016/s0140-6736(00)04376-2 · Cited by 542
In vitro activities of U-100592 and U-100766, novel oxazolidinone antibacterial agents
Zurenko, G. E., Yagi, B. H., Schaadt, R. D., Allison, J. W., Kilburn, J. O., Glickman, S. E., Hutchinson, D. K., Barbachyn, M. R., & Brickner, S. J. (1996) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.40.4.839 · Cited by 461
Self-citationHematologic Effects of Linezolid: Summary of Clinical Experience
Gerson, S. L., Kaplan, S. L., Bruss, J. B., Le, V., Arellano, F. M., Hafkin, B., & Kuter, D. J. (2002) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.46.8.2723-2726.2002 · Cited by 443
Tu, D., Blaha, G., Moore, P. B., & Steitz, T. A. (2005) · Cell · doi:10.1016/j.cell.2005.02.005 · Cited by 433
Cited by
Mendes, R. E., Deshpande, L. M., & Jones, R. N. (2014) · Drug Resistance Updates · doi:10.1016/j.drup.2014.04.002 · Cited by 221
Tedizolid for the Management of Human Infections: In Vitro Characteristics
Locke, J. B., Zurenko, G. E., Shaw, K. J., & Bartizal, K. (2014) · Clinical Infectious Diseases · doi:10.1093/cid/cit616 · Cited by 101
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Metadata
- Authors
- Shaw, K. J., & Barbachyn, M. R.
- Venue
- Annals of the New York Academy of Sciences
- Publisher
- Wiley
- Published
- 2011-12
- Volume
- 1241
- Issue
- 1
- Pages
- 48-70
- ISSN
- 0077-8923 (ISSN-L)
- 1749-6632
- OpenAlex
- W1529101966
- Cited by
- 259
- References
- 92
- FWCI
- 9.60
- Type
- journal article
- Language
- en
- Open access
- closed
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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