chloramphenicol derivatives as antibacterial and anticancer agents: historic problems and current solutions

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ID: 151082
2016
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Abstract
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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dinos2016antibioticschloramphenicol Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors ;George P. Dinos;Constantinos M. Athanassopoulos;Dionissia A. Missiri;Panagiota C. Giannopoulou;Ioannis A. Vlachogiannis;Georgios E. Papadopoulos;Dionissios Papaioannou;Dimitrios L. Kalpaxis
Journal derecho pucp
Year 2016
DOI
10.3390/antibiotics5020020
URL
http://www.mdpi.com/2079-6382/5/2/20
Keywords
antibiotic resistance chloramphenicol antibiotics translation side effects chemical synthesis anticancer agents pharmacology puromycin reactiontherapeutics

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