Abstract
Chloramphenicol (CAM), the bacteriostatic broad-spectrum antibiotic, isolated from Streptomyces venezuelae during the “golden era” of antibiotic discovery, nowadays has limited clinical potential due to adverse side effects and frequent antimicrobial resistance. Numerous CAM analogs were synthesized in order to find the derivatives with improved pharmacological properties and activity on resistant bacterial strains. This work aims to summarize the most recent achievements in obtaining new CAM analogs reported during the last five years. Current investigations are mainly focused on elucidating the molecular basis of the mode of CAM action and determining the mechanisms of resistance to this class of antibiotics or on studies of the possible use of the CAM scaffold to search for therapeutic agents with different CAM modes of action—such as selective antiproliferative agents or bacterial cell wall biosynthesis inhibitors. Hopefully, a deeper understanding of the CAM interactions with the target and its specificity will generate research ideas for developing new effective drugs.
Highlights
Chloramphenicol (CAM) is a bacteriostatic broad-spectrum antibiotic that was isoChloramphenicol is a bacteriostatic broad-spectrum antibiotic that was isolated lated from Streptomyces(CAM)venezuelae in 1947 during the “golden era”of antibiotic discovery fromStreptomyces venezuelae in 1947 during the “golden of antibiotic [1]
Gram-positive caused in thedeveloped extensive countries deformation serious infections, such as caused by Haemophilus influenza, or in patients with bacterial meningitis or brain abscesses who are allergic to other classes of antibiotics, such as penicillins
CAM (1) has a broad spectrum of antibacterial activity, its clinical potential is seriously limited by serious side effects, such as hematologic disorders, immunosuppression, and cancer invasion due to the widely spread antimicrobial resistance to this antibiotic
Summary
Chloramphenicol (CAM) is a bacteriostatic broad-spectrum antibiotic that was isoChloramphenicol is a bacteriostatic broad-spectrum antibiotic that was isolated lated from Streptomyces(CAM). 23S of theof50S of the ribosome prevents the the interaction of an incoming aminoacyl moiety of an aminoacyl-tRNA substrate with interaction of an incoming aminoacyl moiety of an aminoacyl-tRNA substrate with the A the A site [3]. Both hydroxy groups of the antibiotic, as well as the carbonyl group of the dichloroacetamide residue, form a hydrogen bond with the 23S rRNA nucleotides (Figure 1) which results in the inhibition of the peptide bond formation [4]. Published in in mid-2016, exhaustively covered efforts forts to synthesize derivatives with improved pharmacological properties [6].
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