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8-Methyl-7-substituted-1,6-naphthyridine-3-carboxylic acids as New 6-desfluoroquinolone antibacterials

✍ Scribed by Stefano Sabatini; Violetta Cecchetti; Oriana Tabarrini; Arnaldo Fravolini

Publisher: Journal of Heterocyclic Chemistry
Year: 1999
Tongue: English
Weight: 377 KB
Volume: 36
Category: Article
ISSN: 0022-152X
DOI: 10.1002/jhet.5570360422

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✦ Synopsis

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 previous 6‐amino and 6‐hydrogen counterparts, they resulted always less active. However, the presence of methyl group at C‐8 position ensure good Gram‐positive antibacterial activity, with minimum inhibitory concentrations values on the same order of ciprofloxacin for piperidinyl derivative 3d and tetrahydroisoquinolinyl derivative 3c.

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