期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 13, 期 24, 页码 6615-6628出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2005.07.041
关键词
ketolide; N-aryl-alkyl acetamide; 9-iminoether; erythromycin resistant; macrolide; C-11,12 carbonate
A new type of ketolides, bearing an N-aryl-alkyl acetamide moiety at the C-9 iminoether and a cyclic carbonate at the G 11, 12 position was prepared and the antibacterial activities of the compounds were evaluated. Some of the derivatives showed potent antibacterial activity against both Haemophilus influenzae and Streptococcus pneumoniae, which are clinically important respiratory tract pathogens. Among the derivatives prepared, compound 5s with a quinolin-4-yl moiety was found to have potent and well-balanced activity against S. pneumoniae and H. influenzae including erythromycin-resistant strains. (c) 2005 Elsevier Ltd. All rights reserved.
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