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Anhydrolide macrolides. 1. Synthesis and antibacterial activity of 2,3-anhydro-6-O-methyl 11,12-carbamate erythromycin A analogues.

Abstract：

:A series of 3-descladinosyl-2,3-anhydro-6-O-methylerythromycin A 11, 12-carbamate analogues have been synthesized and evaluated for antibacterial activity. These compounds were found to be potent antibacterial agents against Gram-positive organisms in vitro, many having MIC values below 1 microg/mL for the macrolide-susceptible Staphylococcus aureus, Streptococcus pyogenes, and Streptococcus pneumoniae, as well as improved activity compared to erythromycin A against the inducibly MLS (macrolide, lincosamide, and streptogramin B)-resistant organisms. Structure-activity studies revealed that arylalkyl carbamates with two and four carbon atoms between the aromatic moiety and carbamate nitrogen have the best in vitro activity. All of the C-10 epi analogues evaluated were found to have substantially less activity than the corresponding natural C-10 isomer. Several analogues demonstrated moderate antibacterial activity against the constitutively resistant S.aureus A-5278, S. pneumoniae5979, and S.pyogenes 930. However, despite potent in vitro activity, these analogues showed only moderate in vivo activity in mouse protection studies.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Elliott RL,Pireh D,Griesgraber G,Nilius AM,Ewing PJ,Bui MH,Raney PM,Flamm RK,Kim K,Henry RF,Chu DT,Plattner JJ,Or YS

doi

10.1021/jm970547x

subject

Has Abstract

pub_date

1998-05-07 00:00:00

pages

1651-9

issue

10

eissn

0022-2623

issn

1520-4804

pii

jm970547x

journal_volume

41

pub_type

杂志文章

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