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Conformational analysis of ketolide, conformations of RU 004 in solution and bound to bacterial ribosomes.

Abstract：

:A new structurally distinct class of 14-membered-ring macrolides is characterized by a keto-function instead of the cladinose sugar, well-known for its fragility even in weakly acidic media. This new class called ketolides is endowed with remarkable antibacterial activity against macrolide-resistant strains. A complete assignment of the 1H and 13C NMR spectra of RU 004 in deuteriochloroform, methanol-d4 and D2O has been made using different two-dimensional (2D) chemical-shift correlation methods. The study of ketolide-ribosome interaction has been investigated using 2D transferred nuclear Overhauser effect spectroscopy (TRNOESY). A comparison of the conformations in solution and bound to ribosomes was made with those of previous macrolides. This study can highlight some of the significant differences between RU 004 and other antibiotics.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Bertho G,Gharbi-Benarous J,Delaforge M,Lang C,Parent A,Girault JP

doi

10.1021/jm970852i

subject

Has Abstract

pub_date

1998-08-27 00:00:00

pages

3373-86

issue

18

eissn

0022-2623

issn

1520-4804

pii

jm970852i

journal_volume

41

pub_type

杂志文章

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