866954-86-1

Upstream product

• 122-51-0 orthoformic acid triethyl ester 
• 112811-68-4 ethyl 3-methoxy-2,4,5-trifluorobenzoylacetate 
• 136897-64-8 methyl 3-methoxy-2,4,5-trifluorobenzoate 
• 112811-66-2 2,4,5-trifluoro-3-methoxybenzoyl chloride 
• 112811-65-1 3-methoxy-2,4,5-trifluorobenzoic acid 

Relevant academic research and scientific papers

Aminoquinolones as GSK-3 inhibitors

Provided herein are aminoquinolones and pharmaceutically acceptable derivatives thereof. In certain embodiments, provided herein are compounds, compositions and methods for treating, preventing or ameliorating GSK-3 mediated diseases.

A prodrug approach toward the development of water soluble fluoroquinolones and structure-activity relationships of quinoline-3-carboxylic acids

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.