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Chloramphenicol Derivatives as Antibacterial and Anticancer Agents: Historic Problems and Current Solutions
Open accessAbstract
Chloramphenicol (CAM) is the D-threo isomer of a small molecule, consisting of a p-nitrobenzene ring connected to a dichloroacetyl tail through a 2-amino-1,3-propanediol moiety. CAM displays a broad-spectrum bacteriostatic activity by specifically inhibiting the bacterial protein synthesis. In certain but important cases, it also exhibits bactericidal activity, namely against the three most common causes of meningitis, Haemophilus influenzae, Streptococcus pneumoniae and Neisseria meningitidis. Resistance to CAM has been frequently reported and ascribed to a variety of mechanisms. However, the most important concerns that limit its clinical utility relate to side effects such as neurotoxicity and hematologic disorders. In this review, we present previous and current efforts to synthesize CAM derivatives with improved pharmacological properties. In addition, we highlight potentially broader roles of these derivatives in investigating the plasticity of the ribosomal catalytic center, the main target of CAM.
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Lipinski, C. A., Lombardo, F., Dominy, B. W., & Feeney, P. J. (2001) · Advanced Drug Delivery Reviews · doi:10.1016/s0169-409x(00)00129-0 · Cited by 18,139
Organization and regulation of mitochondrial protein synthesis
Ott, M., Amunts, A., & Brown, A. (2016) · Annual Review of Biochemistry · doi:10.1146/annurev-biochem-060815-014334 · Cited by 282
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Metadata
- Authors
- Dinos, G., Athanassopoulos, C., Missiri, D., Giannopoulou, P., Vlachogiannis, I., Papadopoulos, G., Papaioannou, D., & Kalpaxis, D.
- Venue
- Antibiotics
- Publisher
- MDPI AG
- Published
- 2016-06-03
- Volume
- 5
- Issue
- 2
- Pages
- 20
- ISSN
- 2079-6382 (ISSN-L)
- OpenAlex
- W2418036698
- Cited by
- 158
- References
- 2
- FWCI
- 3.76
- Type
- journal article
- Language
- en
- Open access
- gold
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- Dinos, G., Athanassopoulos, C., Missiri, D., Giannopoulou, P., Vlachogiannis, I., Papadopoulos, G., Papaioannou, D., & Kalpaxis, D. (2016). Chloramphenicol Derivatives as Antibacterial and Anticancer Agents: Historic Problems and Current Solutions. Antibiotics. https://doi.org/10.3390/antibiotics5020020
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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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