Recent Trends in Synthesis of Chloramphenicol New Derivatives

Chloramphenicol (CAM), the bacteriostatic broad-spectrum antibiotic, isolated from <i>Streptomyces venezuelae</i> during the “golden era” of antibiotic discovery, nowadays has limited clinical potential due to adverse side effects and frequent antimicrobial resistance. Numerous CAM analo...

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Main Author: Anna N. Tevyashova
Format: Article
Language:English
Published: MDPI AG 2021-03-01
Series:Antibiotics
Subjects:
Online Access:https://www.mdpi.com/2079-6382/10/4/370
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author Anna N. Tevyashova
author_facet Anna N. Tevyashova
author_sort Anna N. Tevyashova
collection DOAJ
description Chloramphenicol (CAM), the bacteriostatic broad-spectrum antibiotic, isolated from <i>Streptomyces venezuelae</i> 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.
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spelling doaj.art-5a0be003a4cd42a7ab78b225e7ab1e522023-11-21T13:38:37ZengMDPI AGAntibiotics2079-63822021-03-0110437010.3390/antibiotics10040370Recent Trends in Synthesis of Chloramphenicol New DerivativesAnna N. Tevyashova0Gause Institute of New Antibiotics, 11 B. Pirogovskaya, 119021 Moscow, RussiaChloramphenicol (CAM), the bacteriostatic broad-spectrum antibiotic, isolated from <i>Streptomyces venezuelae</i> 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.https://www.mdpi.com/2079-6382/10/4/370chloramphenicolsynthesisantibacterial activitypeptidesantibiotic resistanceside effects
spellingShingle Anna N. Tevyashova
Recent Trends in Synthesis of Chloramphenicol New Derivatives
Antibiotics
chloramphenicol
synthesis
antibacterial activity
peptides
antibiotic resistance
side effects
title Recent Trends in Synthesis of Chloramphenicol New Derivatives
title_full Recent Trends in Synthesis of Chloramphenicol New Derivatives
title_fullStr Recent Trends in Synthesis of Chloramphenicol New Derivatives
title_full_unstemmed Recent Trends in Synthesis of Chloramphenicol New Derivatives
title_short Recent Trends in Synthesis of Chloramphenicol New Derivatives
title_sort recent trends in synthesis of chloramphenicol new derivatives
topic chloramphenicol
synthesis
antibacterial activity
peptides
antibiotic resistance
side effects
url https://www.mdpi.com/2079-6382/10/4/370
work_keys_str_mv AT annantevyashova recenttrendsinsynthesisofchloramphenicolnewderivatives