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New 1,8-peri-annelated tricyclic quinolone antibacterials
✍ Scribed by H. Miao; V. Cecchetti; O. Tabarrini; A. Fravolini
- Publisher
- Journal of Heterocyclic Chemistry
- Year
- 2000
- Tongue
- English
- Weight
- 360 KB
- Volume
- 37
- Category
- Article
- ISSN
- 0022-152X
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✦ Synopsis
Abstract
The synthesis of new tricyclic quinolones, resulting from peri‐annelation of 1,2,4‐oxadiazine moiety at the N‐1/C‐8 position of the pharmacophoric quinolone nucleus, are described. None of the synthesized compounds showed interesting antibacterial activity in vitro against the tested strains, with the exception of Klebsiella pneumoniae which was susceptible to all the compounds at MIC values of 8 μg/ml.
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## Abstract 1,6‐Naphthyridine‐8‐methyl‐7‐substituted‐3‐carboxylic acids were synthesized as new 6‐desfluoro‐quinolone antibacterials in which the usual fluorine atom at C‐6 position was replaced by an endocyclic nitrogen atom. Comparing the antibacterial activity of these 6‐azaquinolones with our p