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ketolide : ウィキペディア英語版
ketolide

Ketolides are antibiotics belonging to the macrolide group. Ketolides are derived from erythromycin by substituting the cladinose sugar with a keto-group and attaching a cyclic carbamate group in the lactone ring.〔http://findarticles.com/p/articles/mi_m0PDG/is_4_3/ai_n12417033/ Telithromycin: a brief review of a new ketolide antibiotic. 2004〕 These modifications give ketolides much broader spectrum than other macrolides. Moreover, ketolides are effective against macrolide-resistant bacteria, due to their ability to bind at two sites at the bacterial ribosome as well as having a structural modification that makes them poor substrates for efflux-pump mediated resistance.〔Bertram G. Katzung, Susan B. Masters, Anthony J. Trevor ''Basic & Clinical Pharmacology, 11e'' McGraw-Hill 2009 via "accessmedicine.com"〕 Ketolides block protein synthesis by binding to ribosomal subunits and may also inhibit the formation of newly forming ribosomes. According to a recent study comparing the action
of the classic macrolides
erythromycin and azithromycin
with
ketolides, which are used to treat
serious infections,
the more powerful
drugs (ketolides) were the more "leaky" in
blocking the production of
proteins.
The researchers were surprised to discover
that ketolides, which are known
to be better antibiotics, allow for
many more proteins to be made
compared to the older, less
efficient macrolides.
As a result, it is now believed that allowing
cells to make some proteins
could be much more damaging
for a microbe than not letting it
make any proteins at all.
The findings may point the way
to better and more potent
antibiotics.
The only ketolide on the market at this moment is telithromycin, which is sold under the brand name of Ketek.
Other ketolides in development include cethromycin and solithromycin.
==References==


抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
ウィキペディアで「ketolide」の詳細全文を読む



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