98105-80-7Relevant academic research and scientific papers
7-(substituted)piperazinyl-1-ethyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids
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, (2008/06/13)
7-(substituted)piperazinyl-1-ethyl-6-fluoro-4-oxo-3-quinolinecarboxylic acids, the pharmacologically acceptable salts thereof, compositions containing them, processes and intermediates for producing them, and methods of using them to treat bacterial infections in warm-blooded animals.
UTILISATION DU FLUORURE DE TETRABUTYLAMMONIUM COMME AGENT DE CYCLISATION DANS LA SYNTHESE D'ANTIBACTERIENS DERIVES D'ACIDE PYRIDONE-4-CARBOXYLIQUE-3
Bouzard, D.,Di Cesare, P.,Essiz, M.,Jacquet, J. P.,Remuzon, P.
, p. 1931 - 1934 (2007/10/02)
It has been found that the Bu4NF/THF base/solvent couple is very efficient in the key cyclization step of (2) to (5) in the synthesis of antibacterial pyridonecarboxylic acid derivatives.In particular chiral intermediate (2d) is directly converted in one
Synthesis and Structure-Activity Relationships of Novel Arylfluoroquinolone Antibacterial Agents
Chu, Daniel T. W.,Fernandes, Prabhavathi B.,Claiborne, Akiyo K.,Pihuleac, Eva,Nordeen, Carl W.,et al.
, p. 1558 - 1564 (2007/10/02)
A series of novel arylfluoroquinolones has been prepared.These derivatives are characterized by having a fluorine atom at the 6-position, substituted amino groups at the 7-position, and substituted phenyl groups at the 1-position.Structure-activity relationship (SAR) studies indicate that the in vitro antibacterial potency is greatest when the 1-substituent is either p-fluorophenyl or p-hydroxyphenyl and the 7-substituent is either 1-piperazinyl, 4-methyl-1-piperazinyl, or 3-amino-1-pyrrolidinyl.The electronic and spatial properties of the 1-substituent, as well as the steric bulk, play important roles in the antimicrobial potency in this class of antibacterials.As a result of this study, compounds 45 and 41 were found to possess excellent in vitro potency and in vivo efficacy.
