Synthesis and antibacterial activity of the tricyclic ketolides TE-802 and its analogs

被引：28

作者：

Kashimura, M ^{[1
]}

Asaka, T ^{[1
]}

Misawa, Y ^{[1
]}

Matsumoto, K ^{[1
]}

Morimoto, S ^{[1
]}

机构：

[1] Taisho Pharmaceut Co Ltd, Res Ctr, Omiya, Saitama 3308530, Japan

来源：

JOURNAL OF ANTIBIOTICS | 2001年 / 54卷 / 08期

关键词：

D O I：

10.7164/antibiotics.54.664

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

The novel 6-O-methyl tricyclic ketolides, TE-802 and its analogs were synthesized by two successive cyclization reactions, 11,12-cyclic carbamate formation by intramolecular Michael addition and 9,11-diazaheptene ring construction by intramolecular dehydration reaction. These new tricyclic ketolides exhibited good in vitro antibacterial activity against not only erythromycin-susceptible strains but also erythromycin-resistant Staphylococcus aureus and Streptococcus pneumoniae, which are problematic pathogens of nosocomial and community-acquired respiratory tract infections, respectively.

引用

页码：664 / 678

页数：15

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