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8‐Methyl‐7‐substituted‐1,6‐naphthyridine‐3‐carboxylic acids as New 6‐desfluoroquinolone antibacterials
Author(s) -
Sabatini Stefano,
Cecchetti Violetta,
Tabarrini Oriana,
Fravolini Arnaldo
Publication year - 1999
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.5570360422
Subject(s) - chemistry , ciprofloxacin , nitrogen atom , derivative (finance) , antibiotics , quinolone , antibacterial activity , stereochemistry , carboxylic acid , hydrogen atom , medicinal chemistry , organic chemistry , group (periodic table) , bacteria , biochemistry , biology , financial economics , economics , genetics
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.