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Published on: January 13, 2017
Synthesis and antibacterial activity of the tricyclic ketolides TE-802 and its analogs
M Kashimura1, T Asaka, Y Misawa
1Research Center, Taisho Pharmaceutical Co., Ltd., Saitama, Japan. m.kashimura@po.rd.taisho.co.jp
Abstract:
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.
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