118829-12-2

Upstream product

• 109-72-8 n-butyllithium 
• 327-52-6 1-bromo-2,4,5-trifluorobenzene 
• 124-38-9 carbon dioxide 

Downstream Products

• 2149598-68-3 1-bromo-3-(bromomethyl)-2,4,5-trifluorobenzene 
• 1296310-72-9 (3-bromo-2,5,6-trifluorophenyl)methanol 
• 118829-08-6 1-cyclopropyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6-fluoro-1,4-dihydro-4-oxo-8-(trifluoromethyl)-3-quinolinecarboxylic acid 
• 138059-98-0 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-8-(trifluoromethyl)-3-quinolinecarboxylic acid 
• 118829-20-2 (Z)-3-Cyclopropylamino-2-(2,4,5-trifluoro-3-trifluoromethyl-benzoyl)-acrylic acid ethyl ester 
• 118829-15-5 ethyl 2,4,5-trifluoro-β-oxo-3-(trifluoromethyl)benzenepropanoate 
• 118829-14-4 2,4,5-trifluoro-3-(trifluoromethyl)benzoic acid 
• 118829-18-8 2,4,5-trifluoro-3-trifluoromethylbenzoic acid chloride 
• 118829-13-3 1-bromo-2,4,5-trifluoro-3-(trifluoromethyl)-benzene 

Relevant academic research and scientific papers

Optimization of Blood-Brain Barrier Permeability with Potent and Selective Human Neuronal Nitric Oxide Synthase Inhibitors Having a 2-Aminopyridine Scaffold

Effective delivery of therapeutic drugs into the human brain is one of the most challenging tasks in central nervous system drug development because of the blood-brain barrier (BBB). To overcome the BBB, both passive permeability and efflux transporter liability of a compound must be addressed. Herein, we report our optimization related to BBB penetration of neuronal nitric oxide synthase (nNOS) inhibitors toward the development of new drugs for neurodegenerative diseases. Various approaches, including enhancing lipophilicity and rigidity of new inhibitors and modulating the pKa of amino groups, have been employed. In addition to determining inhibitor potency and selectivity, crystal structures of most newly designed compounds complexed to various nitric oxide synthase isoforms have been determined. We have discovered a new analogue (21), which exhibits not only excellent potency (Ki 30 nM) in nNOS inhibition but also a significantly low P-glycoprotein and breast-cancer-resistant protein substrate liability as indicated by an efflux ratio of 0.8 in the Caco-2 bidirectional assay.

New 8-(trifluoromethyl)-substituted quinolones. The benefits of the 8- fluoro group with reduced phototoxic risk

A series of 8-(trifluoromethyl)-substituted quinolones has been prepared and evaluated for in vitro and in vivo antibacterial activity, and phototolerance in a mouse phototolerance assay. These analogues were compared to the corresponding series of 6,8-di

Antibacterial agents

Novel naphthyridine-, and quinolinecarboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections including the description of certain novel intermediates used in the

8-trifluoromethyl quinolones as antibacterial agents

A novel series of quinolone carboxylic acids for use as antibacterial agents are described. Methods for making the compounds, methods of using the compounds and compositions containing them are also described. Certain novel intermediates are also describe