190839-65-7Relevant academic research and scientific papers
Ketolide Derivatives as Antibacterial Agents
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Page/Page column 6; 11, (2009/01/24)
Provided herein are ketolide derivatives, which can be used as antibacterial agents. Compounds described herein can be used for treating or preventing conditions caused by or contributed to by gram positive, gram negative or anaerobic bacteria, more parti
MACROLIDES DERIVATIVES AS ANTIBACTERIAL AGENTS
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Page/Page column 36, (2010/11/27)
The present invention provides macrolide derivatives, which can be used as antibacterial agents. Compounds described herein can be used for treating or preventing conditions caused by or contributed to by gram-positive, gram-negative or anaerobic bacteria
KETOLIDE DERIVATIVES AS ANTIBACTERIAL AGENTS
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Page/Page column 86-87, (2008/06/13)
The present invention provides ketolide derivatives, which can be used as antibacterial agents. In particular, compounds described herein can be used for treating or preventing conditions caused by or contributed to by Gram-positive, Gram-negative or anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Moraxalla spp., Chlamydia spp., Mycoplasm, Legionella spp., Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Bacillus or Enterobactericeae. Also provided are processes for preparing siuch ketolide derivatives, pharmaceutical compositions thereof, and methods of treating bacterial infections.
KETOLIDE DERIVATIVES AS ANTIBACTERIAL AGENTS
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Page/Page column 24, (2010/11/25)
The present invention provides ketolide derivatives, which can be used as antibacterial agents. In particular, compounds described herein can be used for treating or preventing conditions caused by or contributed to by gram positive, gram negative or anae
Synthesis of 14,15-dehydroerythromycin A ketolides: Effects of the 13-substituent on erythromycin tautomerism
Fardis,Ashley,Carney,Chu
, p. 278 - 284 (2007/10/03)
A ketolide was prepared from 14,15-dehydroerythromycin A by two different routes. The first approach involving oxidation of the 3-OH of 3-descladinosyl-14,15-dehydroerythromycin A 2′-O-acetate gave unexpectedly high levels of 3,11-double oxidation. This may be due to greater formation of the 9,12-hemiketal in 14,15-dehydroerythromycin A and concomitant exposure of the 11-OH group for oxidation. NMR studies of 14,15-dehydroerythromycin A support this hypothesis, revealing a 9:1 ratio of 9-ketone to 9,12-hemiketal in CDC13 and a 1:1 ratio in CD3OD as contrasted with the corresponding tautomer ratios of 30:1 in CDC13, and 6: 1 in CD3OD with erythromycin A. Alteration of the 13-substituent on the erythronolide A ring from ethyl to vinyl thus favors formation of the 9,12-hemiketal. A second route to the ketolides was developed based on these findings, in which the 11-OH is eliminated prior to oxidation of the 3-OH.
