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Pharmacochemical Aspects of the Evolution from Erythromycin to Neomacrolides, Ketolides and Neoketolides
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作者 Ouattara Mahama Coulibaly Songuigama N’Guessan Deto Jean-Paul 《Open Journal of Medicinal Chemistry》 2020年第3期57-112,共56页
Antibiotic macrolides are experiencing renewed interest in anti-infective therapy since the advent of ketolides. This therapeutic class was introduced in order to broaden the narrow antibacterial spectrum of macrolide... Antibiotic macrolides are experiencing renewed interest in anti-infective therapy since the advent of ketolides. This therapeutic class was introduced in order to broaden the narrow antibacterial spectrum of macrolides and to cope with the emergence of germs resistant to Erythromycin A and its hemisynthetic derivatives or neomacrolides (Clarithromycin, Roxithromycin, Azithromycin, Dirithromycin). From a pharmacochemical point of view, ketolides were first of all obtained by operating chemical modulations on Erythromycin A to obtain the neomacrolides, then, by replacing the neutral sugar (<em>L</em>-cladinose) in <em>C</em>3 by a ketone function coupled with the creation of an oxazolidinone like heterocycle in <em>C</em>11 and <em>C</em>12 in place of the hydroxyls present in these positions (Telithromycin, Cethromycin, Solithromycin). These modulations have enabled the improvement of the chemical stability of ketolides in gastric acid medium and increase their affinity for the ribosomal target, hence the broadening of their spectrum of action towards Gram positive germs including strains resistant to other macrolides and to neomacrolides. Therefore, the objective of this systematic review is to report the various pharmacochemical aspects undertaken since 1952 in the macrolide series based on the structure of Erythromycin A. These aspects will focus on the pharmacomodulations that have led, year after year, to the optimization of stability, the improvement of the pharmacodynamic and pharmacokinetic profile and that have allowed the development of neomacrolides, ketolides and neoketolides, which are today essential in the management of severe bronchopulmonary infections. 展开更多
关键词 Pharmacochemistry ERYTHROMYCIN Neomacrolide KETOLIDE Neoketolide Structure-Activity Relationships
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Synthesis of novel 5-O-(6′-O-modified)-desosamine 14-membered ketolides
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作者 Zhehui Zhao Apeng Wang +3 位作者 Xiaoxi Zhang Shuang Yang Zhigang Luo Pingsheng Lei 《Chinese Chemical Letters》 SCIE CAS CSCD 2019年第2期425-427,共3页
A new and facile procedure was developed to synthesize novel 5-0- (6′-O-modified)-desosamine 14-membered ketolides by adopting different protective strategies and comparing various glycosylation conditions. Two trich... A new and facile procedure was developed to synthesize novel 5-0- (6′-O-modified)-desosamine 14-membered ketolides by adopting different protective strategies and comparing various glycosylation conditions. Two trichloroacetimidate donors, with Lev or Ac substituent groups at the C-6 position, were synthesized to couple with the erythronolide. Several novel 5-0- (6′-O-modified)-desosamine 14-membered ketolides were obtained to verify the utility of the method. 展开更多
关键词 ketolides Desosamine Glycosyolation MODIFICATION
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半合成红霉素研究进展 被引量:1
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作者 李兴发 尤启冬 《药学进展》 CAS 2001年第3期138-141,共4页
综述红霉素结构修饰和构效关系研究的新进展 ,介绍其新衍生物 ,特别是以 Ketolides为代表的内酯环 C-3位修饰衍生物 。
关键词 红霉素 结构修饰 ketolides 构效关系
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Research Progress of Ketolide Antibiotics
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作者 邵莉萍 张继瑜 《Agricultural Science & Technology》 CAS 2017年第8期1474-1479,共6页
Macrolide antibiotics have been widely used in clinic due to their good antibacterial effects and high safety, but the drug-resistant bacteria appear constantly. To solve the problem of drug resistance in pathogens, s... Macrolide antibiotics have been widely used in clinic due to their good antibacterial effects and high safety, but the drug-resistant bacteria appear constantly. To solve the problem of drug resistance in pathogens, scholars obtain the third generation of macrolide antibiotics, ketolide antibiotics, which are developed by modifying the structure of macrolide antibiotics, thereby efficiently solving the problem. Ketolide antibiotics are a type of erythromycin derivatives with macrolide structure, and the typical drugs mainly include telithromycin, cethromycin and solithromycin, etc . This paper briefly introduced the recent progress of ketolide antibiotics, with an attempt to provide help to the research and development of new macrolide antibiotics. 展开更多
关键词 Macrolide antibiotics Ketolide antibiotics TELITHROMYCIN Cethromycin Solithromycin PROGRESS
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科技动态
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《国际医药卫生导报》 2001年第4期11-11,共1页
有七十多个国家参加的世界药学会议(FIP)组织在去年底举行的会议上弥漫着对医疗新科技发展忧心重重的气氛。从基因食品管理到基因疾病诊断的应用,一再提醒人们:施法和敬重自然,否则,势将遭自然反扑,让人们自食其果。最典型的范例即来自... 有七十多个国家参加的世界药学会议(FIP)组织在去年底举行的会议上弥漫着对医疗新科技发展忧心重重的气氛。从基因食品管理到基因疾病诊断的应用,一再提醒人们:施法和敬重自然,否则,势将遭自然反扑,让人们自食其果。最典型的范例即来自药物滥用的教训;抗菌素使用泛滥,造成细菌抗药性严重而普遍; 展开更多
关键词 细菌抗药性 人工乳头 药物滥用 ketolides TELITHROMYCIN 疾病诊断 抗菌素使用 新型抗生素 红霉素 基因食品
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抗感染药物:01039 Aventis发表Ketek首批Ⅲ期资料
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作者 金伟华 《国外药讯》 2001年第1期20-21,共2页
在加拿大多伦多第40届抗微生物药与化学疗法跨学科会议(ICAAC)上,Aventis公司发表了其Ketolide抗生素Ketek(telithromycin)(Ⅰ)10项有2500多例临床试验的关键性资料。今年早些时候,公司向美国与欧洲的管理机构提出申请许可证,用于18... 在加拿大多伦多第40届抗微生物药与化学疗法跨学科会议(ICAAC)上,Aventis公司发表了其Ketolide抗生素Ketek(telithromycin)(Ⅰ)10项有2500多例临床试验的关键性资料。今年早些时候,公司向美国与欧洲的管理机构提出申请许可证,用于18岁以上的社区获得性肺炎、慢性支气管炎急性发作及急性鼻窦炎病人与13岁以上的咽炎及扁桃体炎病人,每天给药一次。 展开更多
关键词 抗感染药物 Aventis公司 Ketolide抗生素 临床试验
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