Synthesis and antibacterial activity of 6-O-(heteroaryl-isoxazolyl)propynyl 2-fluoro ketolides.

Tomohiro Sugimoto, Yoichi Shimazaki, Akira Manaka, Tetsuya Tanikawa, Keiko Suzuki, Kayoko Nanaumi, Yoshie Kaneda, Yukiko Yamasaki, 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

Bioorganic & medicinal chemistry letters 2012 Sep 1

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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. Copyright © 2012 Elsevier Ltd. All rights reserved.

Citation

Tomohiro Sugimoto, Yoichi Shimazaki, Akira Manaka, Tetsuya Tanikawa, Keiko Suzuki, Kayoko Nanaumi, Yoshie Kaneda, Yukiko Yamasaki, Hiroyuki Sugiyama. Synthesis and antibacterial activity of 6-O-(heteroaryl-isoxazolyl)propynyl 2-fluoro ketolides. Bioorganic & medicinal chemistry letters. 2012 Sep 1;22(17):5739-43