8Methyl7substituted1,6naphthyridine3carboxylic acids as New 6desfluoroquinolone antibacterialsThis work was previously presented in part: V. Cecchetti, A. Fravolini, M. Palumbo, C. Sissi and O. Tabarrini, First ItalianSwiss Meeting on Medicinal Chemistry, Torino, September 1997, ML20.

Autor: Sabatini, Stefano, Cecchetti, Violetta, Tabarrini, Oriana, Fravolini, Arnaldo
Zdroj: Journal of Heterocyclic Chemistry; July 1999, Vol. 36 Issue: 4 p953-957, 5p
Abstrakt: 1,6Naphthyridine8methyl7substituted3carboxylic acids were synthesized as new 6desfluoroquinolone antibacterials in which the usual fluorine atom at C6 position was replaced by an endocyclic nitrogen atom. Comparing the antibacterial activity of these 6azaquinolones with our previous 6amino and 6hydrogen counterparts, they resulted always less active. However, the presence of methyl group at C8 position ensure good Grampositive antibacterial activity, with minimum inhibitory concentrations values on the same order of ciprofloxacin for piperidinyl derivative 3d and tetrahydroisoquinolinyl derivative 3c.
Databáze: Supplemental Index