108129-55-1

Upstream product

• 118-93-4 o-hydroxyacetophenone 
• 50-80-6 5-amino-2-hydroxyacetophenone 
• 7298-67-1 5-acetamido-2-hydroxyacetophenone 
• 1450-76-6 1-(2-hydroxy-5-nitrophenyl)ethanone 
• 70978-41-5 5-acetamido-2-hydroxy-3-nitroacetophenone 

Downstream Products

• 199460-09-8 4',8-diaminoflavone 
• 1027904-08-0 1-(2-Hydroxy-3-nitro-phenyl)-3-(4-nitro-phenyl)-propane-1,3-dione 
• 158555-12-5 4',8-dinitroflavone 
• 28177-69-7 2-hydroxy-3-nitroacetophenone 

Relevant academic research and scientific papers

N-sulfamoyl-N'-benzopyranpiperidine compounds and uses thereof

N-sulfamoyl-N′-benzopyranpiperidine compounds of formula I and their physiologically acceptable acid addition salts, pharmaceutical compositions comprising them, processes for their preparation, and their use for the treatment and/or inhibition of glaucoma, epilepsy, bipolar disorders, migraine, neuropathic pain, obesity, type II diabetes, metabolic syndrome, alcohol dependence, and/or cancer, and related concomitant and/or secondary diseases or conditions.

N-SULFAMOYL-N’-BENZOPYRANPIPERIDINES AS INHBITORS OF CARBONIC ANHYDRASES

The present invention relates to novel N-sulfamoyl-N'-benzopyranpiperidines of general formula (I) and their physiologically acceptable acid addition salts, to pharmaceutical compositions comprising them, processes for their preparation, and their use for the prophylaxis and/or treatment and/or prevention and/or inhibition of glaucoma, epilepsy, bipolar disorders, migraine, neuropathic pain, obesity, type II diabetes, metabolic syndrome, alcohol dependence, and/or cancer, and its concomitant and/or secondary diseases or conditions.

Synthesis and Biochemical Evaluation of a Series of Aminoflavones as Potential Inhibitors of Protein-Tyrosine Kinases p56lek, EGFr, and p60v-src

A series of nitroflavones, 8a-p, and their corresponding aminoflavone hydrochloride salts, 10a-p, was synthesized.The preparation of nitroflavones 8b-i,o,p began with commercially available o-hydroxyacetophenones 2b-f which were converted to o-hydroxynitroacetophenones 3a-h via a variety of nitration methods, followed by condensation with nitrobenzyl chlorides and cyclization under acidic condition.The nitroflavones 8a,j-n were prepared by nitration of the corresponding flavones 7a-e.These new compounds were evaluated for their abilities to inhibit the in vitro protein-tyrosine kinase activities of p56lek, EGFr, and p60v-src, and all of the active compounds were amino-substituted flavones.None of the nitroflavones inhibited the enzymes.The most active substance in this series against p56lek was compound 10j, which had an IC50 of 18 μM.When tested versus EGFr, compounds 10a,m displayed IC50's of 8.7 and 7.8 μM, respectively.Against p60v-src, 10a,m showed IC50 values of 28.8 and 38.4 μM, respectively.