Paper
Chloramphenicol Derivatives as Antibacterial and Anticancer Agents: Historic Problems and Current Solutions
Published Jun 1, 2016 · G. Dinos, C. Athanassopoulos, Dionissia A. Missiri
Antibiotics
119
Citations
4
Influential Citations
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.
Highly CitedChloramphenicol derivatives show potential as antibacterial and anticancer agents, but current efforts focus on improving pharmacological properties and addressing side effects like neurotoxicity and hematologic disorders.
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