641639-48-7

Upstream product

• 63-74-1 sulfanilamide 
• 113503-90-5 2-hydroxy-4-oxo-4-p-tolylbut-2-enoic acid ethyl ester 
• 122-00-9 para-methylacetophenone 
• 170569-23-0 1-(4-sulfamoylphenyl)-5-p-tolyl-1H-pyrazole-3-carboxylic acid ethyl ester 
• 170571-25-2 methyl 1-(4-sulfamoylphenyl)-5-(p-tolyl)-1H-pyrazole-3-carboxylate 

Downstream Products

• 1287761-20-9 (E)-3-[1-(4-sulfamoylphenyl)-5-p-tolyl-1H-pyrazol-3-yl]-acrylic acid ethyl ester 
• 1287761-21-0 3-[1-(4-sulfamoylphenyl)-5-p-tolyl-1H-pyrazol-3-yl]-propionic acid ethyl ester 
• 1287761-22-1 4-[3-(3-hydroxypropyl)-5-p-tolyl-pyrazol-1-yl]-benzenesulfonamide 
• 1287761-23-2 4-{3-[3-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-propyl]-5-p-tolyl-pyrazol-1-yl}-benzenesulfonamide 
• 1287761-24-3 C₁₉H₂₂N₄O₂S 
• 1287760-95-5 4-(5-p-tolyl-3-{3-[3-(3-trifluoromethylphenyl)-ureido]-propyl}-pyrazol-1-yl)-benzenesulfonamide 
• 960215-02-5 3-[1-(4-sulfamoylphenyl)-5-p-tolyl-1H-pyrazol-3-yl]propanoic acid 
• 850829-14-0 4-(3-formyl-5-p-tolyl-pyrazol-1-yl)-benzenesulfonamide 

Relevant academic research and scientific papers

Novel (pyrazolyl)benzenesulfonamides with a nitric oxide-releasing moiety as selective cyclooxygenase-2 inhibitors

Abstract Inhibition of cyclooxygenase-2 (COX-2) is a promising anti-inflammatory therapeutic strategy, but long-term medication with COX-2-inhibitors (coxibs) may be associated with adverse cardiovascular effects. Functionalization of existing lead struct

PYRAZOLE INHIBITORS OF COX-2 AND SEH

The present invention provides compounds and compositions, e.g., a series of compounds wherein a 1,5-biarylpyrazole group is conjugated to a urea group by a non-cleavable covalent chain, that are useful as dual COX-2/sEH inhibitors. The compounds disclosed herein have activity associated with the arachidonate cascade. The activity of these compounds was demonstrated using a lipopolysaccharide (LPS) induced model of pain in the rat. The compounds of the present invention demonstrated superior anti-allodynic activity as compared to the same dose of celecoxib, i.e., a COX-2 inhibitor, also as compared to the same dose of t-AUCB, i.e., a sEH inhibitor, and also as compared to the co-administered same dose of both celecoxib and t-AUCB. The dual inhibitors of the present invention demonstrate enhanced in vivo anti-allodynic activity in a nociceptive behavioral assay. In addition, the compounds of the present invention also demonstrated to have potent anti-angiogenic effects toward endothelial cells (HUVEC) and inhibit angiogenesis in vitro, ex vivo and in vivo. The dual inhibitors of the present invention also demonstrate anti-angiogenic effect to slow breast tumor growth in vivo.

New selective carbonic anhydrase IX inhibitors: Synthesis and pharmacological evaluation of diarylpyrazole-benzenesulfonamides

Carbonic anhydrase (CA) IX expression is increased upon hypoxia and has been proposed as a therapeutic target since it has been associated with poor prognosis, tumor progression and pH regulation. We report the synthesis and the pharmacological evaluation

Synthesis and structure-activity relationship studies of urea-containing pyrazoles as dual inhibitors of cyclooxygenase-2 and soluble epoxide hydrolase

A series of dual inhibitors containing a 1,5-diarylpyrazole and a urea were designed, synthesized, and evaluated as novel COX-2/sEH dual inhibitors in vitro using recombinant enzyme assays and in vivo using a lipopolysaccharide (LPS) induced model of pain in rats. The best inhibition potencies and selectivity for sEH and COX-2 over COX-1 were obtained with compounds (21b, 21i, and 21j) in which both the 1,5-diaryl-pyrazole group and the urea group are linked with a three-methylene group. Compound 21i showed the best pharmacokinetic profiles in both mice and rats (higher AUC and longer half-life). Following subcutaneous administration at 10 mg/kg, compound 21i exhibited antiallodynic activity that is more effective than the same dose of either a COX-2 inhibitor (celecoxib) or a sEH inhibitor (t-AUCB) alone, as well as coadministration of both inhibitors. Thus, these novel dual inhibitors exhibited enhanced in vivo antiallodynic activity in a nociceptive behavioral assay.

LARGE CONDUCTANCE CALCIUM-ACTIVATED K CHANNEL OPENER

The present invention provides a large conductance calcium-activated K channel opener comprising a compound of the formula (I): wherein R1 and R3 are each sulfonamide, carbamoyl, acyl, amino, and the like, m and n are each 0 to 2, R2 and R4 are each cyano, nitro, hydroxyl, an alkoxy, a halogen, or an alkyl, Ring A is benzene or a heterocyclic ring, Ring B is benzene, a heterocyclic ring, a cycloalkane etc, and Ring Q is pyrazole or isoxazole, or a pharmaceutically acceptable salt thereof as an active ingredient.