20012-60-6

Upstream product

• 95-55-6 2-amino-phenol 
• 85-44-9 phthalic anhydride 

Downstream Products

• 20012-63-9 o-(benzyloxy)aniline 
• 1289486-03-8 2-(benzyloxy)-N-(3-(4-methoxytetrahydro-2H-pyran-4-yl) benzyl) aniline 
• 1289485-93-3 N-(2-(benzyloxy)phenyl)-N-(3-(4-methoxytetrahydro-2H-pyran-4-yl)benzyl)methanesulfonamide 
• 1289485-83-1 N-(2-(benzyloxy)phenyl)-1-(3-(4-methoxytetrahydro-2H-pyran-4-yl)phenyl)methanesulfonamide 
• 1289485-65-9 N-(2-(benzyloxy)phenyl)methanesulfonamide 
• 127817-82-7 2-Benzyloxy-N-methyl-4'-nitro-3'-trifluormethyldiphenylamin 
• 127817-79-2 2-Benzyloxy-4'-nitro-3'-trifluormethyldiphenylamin 
• 127817-84-9 2-Hydroxy-N-methyl-4'-nitro-3'-trifluormethyldiphenylamin 
• 127817-83-8 2-Hydroxy-4'-nitro-3'-trifluormethyldiphenylamin 

Relevant academic research and scientific papers

Syntheses and characterization of nimesulide derivatives for dual enzyme inhibitors of both cyclooxygenase-1/2 and 5-lipoxygenase

Cyclooxygenase-1/2 (COX-1/2) and 5-lipoxygenase (5-LOX) are enzymes in two different pathways in the inflammatory process. In the present study, a variety of new nimesulide derivatives were synthesized through incorporation of a 5-LOX pharmacophore into nimesulide followed with some structural modifications, which were then characterized for dual enzyme inhibitors for these two types of enzymes. Their structure-activity relationships (SARs) were studied, and compound 20f was found to be an excellent dual enzyme inhibitor. Its binding conformation and interaction mode were studied with molecular docking experiments. Compound 20f could become a lead compound for further development for potential anti-inflammatory drugs.

Development of nonsteroidal antiandrogens: 4-Nitro-3-trifluoro-methyldiphenylamines

For the development of new nonsteroidal antiandrogens a series of 4-nitro-3-trifluoromethyldiphenylamines was synthesized and compounds were tested for their affinities to steroid hormone receptors and for antiandrogenic activities. These compounds were synthesized by reacting 4-nitro-3-trifluoromethylphenylsulfocyanamide-sodium (4) with the corresponding aromatic amines to give the N-(4-nitro-3-trifluoromethylphenylsulfonyl)-N'-phenylguanidines. The crude products were then converted to the desired diphenylamines by Smiles rearrangement and hydrolysis. 2-Hydroxy-4'-nitro-3'-trifluoromethyldiphenylamine (13), which shows a relative binding affinity (RBA) to the androgen receptor (AR) of 6.5% of that of testosterone, exerts a higher affinity than hydroxyflutamide (RBA = 4.5). Shift of the hydroxy-function to position 3 or 4 as well as N-methylation caused a decrease in AR-affinity. Compounds exerting AR-affinity were tested for antiandrogenic activity. Compound 13 showed the best antiandrogenic effect, though less than the well-known antiandrogen flutamide.