Online article for Non-subscribers

Pay per view

Heterocycles has a pay-per-view service for Non-subscribers.
You will be able to directly purchase the full text article through PayPal.
Your purchased Paper can be downloaded after the payment is completed.
An e-mail will be sent the URL to download the paper.
If you have any questions, please contact:

Price: ¥ 4,400 (Yen only)
Period: This Article can be accessed for 7 days.

Paper | Regular issue | Vol 96, No. 5, 2018, pp.858-881
Published online, 20th April, 2018
DOI: 10.3987/COM-18-13889
Design, Synthesis, and Biological Evaluation of Novel 8-Methoxyquinolones Bearing Fused Pyrrolidinyl Moieties at the C-7 Position with Potent Antibacterial Activity Against Respiratory Pathogens

Takashi Odagiri,* Hiroaki Inagaki, Masatoshi Nagamochi, Takahiro Kitamura, Satoshi Komoriya, and Hisashi Takahashi

*R&D Division, Daiichi Sankyo CO., Ltd, 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan


Novel 8-methoxyquinolones bearing fused pyrrolidinyl moieties at the C-7 position were designed, synthesized, and evaluated for their potent antibacterial activity for the treatment of respiratory tract infections. Compound 5, possessing a trans-fused octahydroisoindole ring at the C-7 position of the quinolone scaffold, exhibited potent in vitro antibacterial activity against nosocomial respiratory pathogens including levofloxacin-resistant Escherichia coli and methicillin-resistant Staphylococcus aureus strains. Furthermore, compound 5 showed a favorable pharmacokinetic profile after a single oral administration in rats.