96568-05-7Relevant articles and documents
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety
Huang, Ju,Wang, Minghua,Wang, Bin,Wu, Zhaoyang,Liu, Mingliang,Feng, Lianshun,Zhang, Jun,Li, Xiaoning,Yang, Yang,Lu, Yu
, p. 2262 - 2267 (2016/04/20)
A series of novel 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety were synthesized and evaluated for their biological activity. Our results reveal that compounds 9a-9c have considerable activity against both of MTB H37Rv ATCC 27294 (MICs: 3.81-7.13 μg/mL) and methicillin-sensitive Staphylococcus aureus strains (MICs: 0.008-0.5 μg/mL).
Fluoronaphthyridines as Antibacterial Agents. 4. Synthesis and Structure-Activity Relationships of 5-Substituted-6-fluoro-7-(cycloalkylamino)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic Acids
Bouzard, D.,Cesare, P. Di,Essiz, M.,Jacquet, J. P.,Ledoussal, B.,et al.
, p. 518 - 525 (2007/10/02)
A series of 5-substituted-6-fluoro-7-(cycloalkylamino)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids have been prepared and tested for their in vitro and in vivo antibacterial activities.The 5-methyl group gave better in vitro activity with the 1-cyclopropyl appendage, but poorer activity with the 1-tert-butyl moiety.With the 1-(2,4-difluorophenyl) substitution, the influence of the 7-cycloalkylamino group was determinant: a (3S)-3-aminopyrrolidine was shown to enhance greatly the in vitro and in vivo activity of the 5-methyl derivative.Compound 33 (BMY 43748) was selec ted as a promising candidate for an improved therapeutic agent.