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氯霉素新衍生物合成的最新趋势

Recent Trends in Synthesis of Chloramphenicol New Derivatives.

作者信息

Tevyashova Anna N

机构信息

Gause Institute of New Antibiotics, 11 B. Pirogovskaya, 119021 Moscow, Russia.

出版信息

Antibiotics (Basel). 2021 Mar 31;10(4):370. doi: 10.3390/antibiotics10040370.

DOI:10.3390/antibiotics10040370
PMID:33807439
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8066525/
Abstract

Chloramphenicol (CAM), the bacteriostatic broad-spectrum antibiotic, isolated from 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.

摘要

氯霉素（CAM）是一种抑菌性广谱抗生素，在抗生素发现的“黄金时代”被分离出来，如今由于其副作用和频繁的抗菌耐药性，临床应用潜力有限。为了找到具有改善药理特性和对耐药菌株活性的衍生物，人们合成了许多氯霉素类似物。这项工作旨在总结过去五年中报道的在获得新型氯霉素类似物方面的最新成果。目前的研究主要集中在阐明氯霉素作用模式的分子基础，确定对这类抗生素的耐药机制，或者研究利用氯霉素骨架寻找具有不同氯霉素作用模式的治疗剂，如选择性抗增殖剂或细菌细胞壁生物合成抑制剂。希望对氯霉素与靶点相互作用及其特异性的更深入理解能为开发新的有效药物产生研究思路。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5178/8066525/f12b2ae6faba/antibiotics-10-00370-sch008.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5178/8066525/94d0b9886a8c/antibiotics-10-00370-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5178/8066525/58962a6c2f5e/antibiotics-10-00370-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5178/8066525/203dea479975/antibiotics-10-00370-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5178/8066525/7fbab93f8f16/antibiotics-10-00370-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5178/8066525/f71463c034b2/antibiotics-10-00370-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5178/8066525/ffbc9d9ab403/antibiotics-10-00370-sch003.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5178/8066525/b0b512300f5b/antibiotics-10-00370-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5178/8066525/e7de9bb69a4b/antibiotics-10-00370-sch005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5178/8066525/ef5f5e0d0c1c/antibiotics-10-00370-sch006.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5178/8066525/2a0fa7453656/antibiotics-10-00370-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5178/8066525/f12b2ae6faba/antibiotics-10-00370-sch008.jpg

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