970-12-7

Upstream product

• 4392-54-5 4-aminosulfonylphenylhydrazine 
• 93-91-4 1-phenylbutan-1,3-dione 
• 17852-52-7 4-hydrazinobenzene-1-sulfonamide hydrochloride 
• 1817-57-8 4-phenyl-3-butyne-2-one 
• 80883-88-1 C₁₆H₁₇N₃O₂S 
• 80883-90-5 4-(3-methyl-5-phenyl-4,5-dihydro-1H-pyrazol-1-yl)benzenesulfonamide 
• 122-57-6 1-Phenylbut-1-en-3-one 
• 100-52-7 benzaldehyde 

Downstream Products

• 78794-40-8 C₂₄H₂₂N₄O₂S₂ 
• 78794-39-5 C₂₄H₂₂N₄O₂S₂ 
• 78794-38-4 C₂₃H₂₆N₄O₂S₂ 
• 78794-37-3 C₂₁H₂₄N₄O₂S₂ 
• 78794-35-1 C₁₉H₂₀N₄O₂S₂ 
• 586333-65-5 5-phenyl-1-(4-sulfamoylphenyl)-1H-pyrazole-3-carboxylic acid 
• 78794-41-9 1-(p-sulfamylphenyl)-4-bromo-3-methyl-5-phenylpyrazole 
• 78794-48-6 C₁₉H₁₉BrN₄O₂S₂ 
• 78794-50-0 C₂₁H₂₃BrN₄O₂S₂ 
• 78794-52-2 C₂₄H₂₁BrN₄O₂S₂ 
• 78794-53-3 C₂₄H₂₁BrN₄O₂S₂ 
• 78794-51-1 C₂₃H₂₅BrN₄O₂S₂ 

Relevant academic research and scientific papers

Inhibition of carbonic anhydrase II by sulfonamide derivatives

A series of sulfonamide derivatives were synthesized, and the enzyme inhibitory activity of the synthesized compounds on carbonic anhydrase II was evaluated. Through molecular docking studies, it was found that compounds 1b, 1e, 2a, 2b, 3a have a strong binding affinity to carbonic anhydrase II. The IC50 values of the four compounds 1e, 2b, 3a, and 3b were lower than that of the positive control drug acetazolamide. What’s more, the compounds had a high inhibitory activity for A549 lung cancer cell growth, among them, 1e and 3a could inhibit both carbonic anhydrase II and lung cancer cell proliferation.

Design, synthesis and biological evaluation of novel diaryl pyrazole derivatives as anticancer agents

Cancer is one of the major causes of mortality all around the world. Globally, nearly 1 in 6 deaths is due to cancer. Researchers are trying to synthesize new anticancer agents. Previous studies demonstrated that some pyrazole derivatives could be considered as potential anticancer agents. Herein, ten novel derivatives of 1,5-diarylpyrazole were synthesized in four step reactions and cytotoxic activity was investigated by MTT cell viability assay. All of the compounds were characterized by1H NMR and13C NMR and their purity was confirmed by elemental analysis. The cytotoxicity was determined against three cancerous cell lines (HT-29, U87MG and MDA-MB 468) and AGO1522 as a normal cell line. Compound 5a showed the best cytotoxic activity on cancerous cell lines in comparison to paclitaxel. Annexin V/ PI staining assay also showed that compounds 5a and 5i would lead to significant apoptosis induction in MDA-MB 486 cell line.

Synthesis of pyrazolones and pyrazoles via Pd-catalyzed aerobic oxidative dehydrogenation

A palladium-catalyzed oxidative dehydrogenation reaction in the presence of AMS and base to synthesize pyrazolones and pyrazoles was identified. This method can be utilized to a wide range of substrates, operates under mild react conditions and can give high yields. We believe it could be used as an alternative protocol for the classical dehydrogenation reactions.

Synthesis of tri- and tetrasubstituted pyrazoles via Ru(II) catalysis: Intramolecular aerobic oxidative C-N coupling

An unprecedented ruthenium(II)-catalyzed intramolecular oxidative C-N coupling method has been developed for the facile synthesis of a variety of synthetically challenging tri- and tetrasubstituted pyrazoles. Dioxygen gas is employed as the oxidant in this transformation. The reaction demonstrates excellent reactivity, functional group tolerance, and high yields.

Highly regioselective synthesis of 1-aryl-3,4,5-substituted pyrazoles

A highly regioselective synthesis of 1-aryl-3,4,5-substituted pyrazoles based on the condensation of 1,3-diketones with arylhydrazines is described. The reaction proceeds at room temperature in N,N-dimethylacetamide and furnishes pyrazoles in 59-98% yield

Processes for the preparation of 1,5-diaryl-3-substituted-pyrazoles

Provided are processes and chemical intermediates useful for preparing a compound of the formula I wherein X is selected from the group consisting of C1-C6 trihalomethyl; C1-C6 alkyl; and an optionally substituted or di-substituted phenyl group of formula II: Y and Z are independently selected from the group consisting of substituted and unsubstiotuted aryl

Substituted pyrazolyl benzenesulfonamides for use in veterinary therapies

A method of using pyrazolyl benzenesulfonamide compounds in treating inflammation and inflammation-related disorders in companion animals is disclosed.

Substituted pyrazolyl benzenesulfonamides for the treatment of inflammation

A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: STR1 or a pharmaceutically-acceptable salt thereof.

Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: Identification of 4-[5-(4-methylphenyl)- 3(trifluoromethyl)-1h-pyrazol-1-yl]benzenesulfonamide (sc-58635, celecoxib)

A series of sulfonamide-containing 1,5-diarylpyrazole derivatives were prepared and evaluated for their ability to block cyclooxygenase-2 (COX-2) in vitro and in vivo. Extensive structure-activity relationship (SAR) work was carried out within this series, and a number of potent and selective inhibitors of COX-2 were identified. Since an early structural lead (1f, SC- 236) exhibited an unacceptably long plasma half-life, a number of pyrazole analogs containing potential metabolic sites were evaluated further in vivo in an effort to identify compounds with acceptable pharmacokinetic profiles. This work led to the identification of 1i (4-[5-(4-methylphenyl)-3- (trifluoromethyl)-1H-pyrazol-1-y1]benzenesulfonamide, SC-58635, celecoxib), which is currently in phase III clinical trials for the treatment of rheumatoid arthritis and osteoarthritis.