103995-00-2Relevant academic research and scientific papers
A prodrug approach toward the development of water soluble fluoroquinolones and structure-activity relationships of quinoline-3-carboxylic acids
Baker, William R.,Cai, Shaopei,Dimitroff, Martin,Fang, Liming,Huh, Kay K.,Ryckman, David R.,Shang, Xiao,Shawar, Ribhi M.,Therrien, Joseph H.
, p. 4693 - 4709 (2007/10/03)
A fluoroquinolone prodrug, PA2808, was prepared and shown to convert to the highly active parent drug PA2789. In vitro and in vivo activation of PA2808 by alkaline phosphatase was demonstrated using disk diffusion and rat lung infection models. The water solubility of PA2808 showed a marked increase compared to PA2789 over a pH range suitable for aerosol drug delivery. A total of 48 analogues based on PA2789 were prepared and screened against a panel of Gram-positive and Gram-negative pathogens. Incorporating a cyclopropane-fused pyrrolidine (amine g) at C-7 resulted in some of the most active analogues.
Antimicrobial 1-substituted phenyl-4-oxoquinoline-3-carboxylic acid compounds and compositions thereof
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, (2008/06/13)
Novel 1-substituted phenyl-4-oxoquinoline-3-carboxylic acid compounds of the formula: STR1 wherein R is hydrogen atom or fluorine atom, R° is hydroxy, fluorine atom or an alkanoyloxy having 1 to 6 carbon atoms, and X1 is hydrogen atom or fluorine atom, and a pharmaceutically acceptable salt thereof, said compounds having excellent antimicrobial activity and hence being useful as an antimicrobial agent, and a pharmaceutical composition comprising as an active ingredient said 1-substituted phenyl-4-oxoquinoline-3-carboxylic acid compounds or a pharmaceutically acceptable salt thereof in admixture with a pharmaceutically acceptable diluent or carrier.
