- A facile and scaleable synthesis of 3-O-decladinose-6-methyl-10,11- dehydrate-erythromycin-3-one-2′-acetate, an important intermediate for ketolide synthesis
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A facile and scaleable synthetic process of compound 2, an important intermediate for synthesis of ketolide semisynthetic antibiotics, was developed starting from commercially available clathromycin with an overall yield of ~74%. This synthetic pathway wa
- Wei, Xin,You, Qidong
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- Synthesis and antibacterial evaluation of novel 11-O-aralkylcarbamoyl-3-O-descladinosylclarithromycin derivatives
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A series of novel 11-O-aralkylcarbamoyl-3-O-descladinosylclarithromycin derivatives were designed, synthesized and evaluated for their in vitro antibacterial activity. The results showed that the majority of the target compounds displayed potent activity against erythromycin-susceptible S. pyogenes, erythromycin-resistant S. pneumoniae A22072 expressing the mef gene and S. pneumoniae AB11 expressing the mef and erm genes. Besides, most of the target compounds exhibited moderate activity against erythromycin-susceptible S. aureus ATCC25923 and B. subtilis ATCC9372. In particular, compounds 11a, 11b, 11c, 11e, 11f and 11h were found to exert favorable antibacterial activity against erythromycin-susceptible S. pyogenes with the MIC values of 0.015–0.125 μg/mL. Furthermore, compounds 10e, 11a, 11b and 11c showed superior activity against erythromycin-resistant S. pneumoniae A22072 with the MIC values of 0.25–0.5 μg/mL. Additionally, compound 11c was the most effective against all the erythromycin-resistant S. pneumoniae strains (A22072, B1 and AB11), exhibiting 8-, 8- and 32-fold more potent activity than clarithromycin, respectively.
- Jia, Li,Wang, Yinhu,Wang, Yanxia,Qin, Yinhui,Hu, Chaoyu,Sheng, Juzheng,Ma, Shutao
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p. 2471 - 2476
(2018/06/06)
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- Synthesis and antibacterial activity of novel ketolides with 11,12-quinoylalkyl side chains
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A series of quinoylalkyl side chains was designed and synthesized, followed by introduction into ketolides by coupling with building block 6 or 32. The corresponding targets 7a–n, 33b, and 33e were tested for their in vitro activities against a series of macrolide-sensitive and macrolide-resistant pathogens. Some of them showed a similar antibacterial spectrum and comparable activity to telithromycin. Among them, two C2-F ketolides, compounds 33b and 33e, displayed excellent activities against macrolide-sensitive and macrolide-resistant pathogens.
- Zhao, Zhe-hui,Zhang, Xiao-xi,Jin, Long-long,Yang, Shuang,Lei, Ping-sheng
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p. 2358 - 2363
(2018/06/25)
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- Erythromycin A ketone antibiotic derivative and preparation method and application thereof
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The invention discloses an erythromycin A ketone antibiotic derivative containing substituted quinoline or isoquinoline, a preparation method and application of the erythromycin A ketone antibiotic derivative, and a compound side-chain intermediate and a synthetic method. The key point is that the compound indicated in the formula I has efficacy of broad-spectrum antibiotics and antibacterial activity and anti-resistant bacterial activity which are capable of inhibiting gram-positive bacteria and gram-negative bacteria. The compound can serve as the broad-spectrum antibiotics, and meanwhile, antibacterial and antiviral activity of gram-positive bacteria and gram-negative bacteria are inhibited.
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- Erythromycin A ketolide antibiotic derivatives containing quinoline substituent group, and preparation methods and applications thereof
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The invention discloses a series of erythromycin A ketolide antibiotic derivatives containing quinoline substituent group, represented by a formula I. The invention also provides preparation methods and applications of the derivatives, and side-chain inte
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Paragraph 0297; 0298
(2016/10/08)
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- Synthesis and antibacterial activity of novel ketolides with 11,12-sulfur contained aryl alkyl side chains
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A novel series of ketolides with 11,12-sulfur contained aryl alkyl side chains were synthesized and evaluated for their antibacterial activity. These ketolides exhibited potent activity against key macrolide sensitive and resistant respiratory pathogens.
- Chen, Xiao-Zhuo,Xu, Peng,Liu, Lu,Zheng, Dan,Lei, Ping-Sheng
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scheme or table
p. 208 - 217
(2011/02/26)
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