title: Synthesis and antibacterial activity of 5-methoxy- and 5-hydroxy-6-fluoro-1,8-naphthyridone-3-carboxylic acid derivatives.
abstract: A series of 5-methoxy- and 5-hydroxy-6-fluoro-1,8-naphthyridone-3-carboxylic acid derivatives were prepared and evaluated for cell-free bacterial protein synthesis inhibition and whole cell antibacterial activity. When compared to the analogous 5-hydrogen compounds, the presence of the 5-OH group negatively affects biochemical potency. However, a tolerance of the 5-methoxy group is indicated. Only moderate whole cell antibacterial activity is seen, but this could be due to poor cellular penetration. Because only a few 7-position variants were made for this study, further investigation into this novel series combining a broader range of 7-amino derivatives with these 5-position modifications is warranted.
authors.affiliation: Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA. mathew.hansen@abbott.com
authors.forename: T
authors.initials: T
authors.lastname: Matthew Hansen
authors.forename: Yu-Gui
authors.initials: YG
authors.lastname: Gu
authors.forename: Tamara M
authors.initials: TM
authors.lastname: Rehm
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Dandliker
authors.forename: Linda E
authors.initials: LE
authors.lastname: Chovan
authors.forename: Mai H
authors.initials: MH
authors.lastname: Bui
authors.forename: Angela M
authors.initials: AM
authors.lastname: Nilius
authors.forename: Bruce A
authors.initials: BA
authors.lastname: Beutel
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002264:Carboxylic Acids / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D002264:Carboxylic Acids