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Synthesis and antibacterial activity of 6-O-(heteroaryl-isoxazolyl)propynyl 2-fluoro ketolides. 2012
Tomohiro Sugimoto, and
Yoichi Shimazaki, and
Akira Manaka, and
Tetsuya Tanikawa, and
Keiko Suzuki, and
Kayoko Nanaumi, and
Yoshie Kaneda, and
Yukiko Yamasaki, and
Hiroyuki Sugiyama
Medicinal Research Laboratories, Taisho Pharmaceutical Co. Ltd, 1-403 Yoshino-cho, Kita-ku, Saitama-shi, Saitama 331-9530, Japan. tomohiro.sugimoto@po.rd.taisho.co.jp
Macrolide antibiotics are widely prescribed for the treatment of respiratory tract infections; however, the increasing prevalence of macrolide-resistant pathogens is a public health concern. Therefore, the development of new macrolide derivatives with activities against resistant pathogens is urgently needed. A series of novel 6-O-(heteroaryl-isoxazolyl)propynyl 2-fluoro ketolides has been synthesized from erythromycin A. These compounds have shown very promising in vitro and in vivo antibacterial activities against key respiratory pathogens including erythromycin-susceptible/resistant strains.
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