1293980-75-2

Upstream product

• 4392-54-5 4-aminosulfonylphenylhydrazine 
• 100-06-1 1-(4-methoxyphenyl)ethanone 
• 17852-52-7 4-hydrazinobenzene-1-sulfonamide hydrochloride 

Downstream Products

• 1293980-80-9 4-[4-formyl-3-(4-methoxyphenyl)-1H-pyrazol-1-yl]benzenesulfonamide 
• 1293980-85-4 1-[4-(aminosulfonyl)phenyl]-3-(4-methoxyphenyl)-1H-pyrazole-4-carboxylic acid 
• 1293980-91-2 4-[4-cyano-3-(4-methoxyphenyl)-1H-pyrazol-1-yl]benzenesulfonamide 
• 1293980-98-9 1-[4-(aminosulfonyl)phenyl]-3-(4-methoxyphenyl)-1H-pyrazole-4-carbothioamide 
• 1293980-77-4 N-[(dimethylamino)methylidene]-4-[4-formyl-3-(4-methoxyphenyl)-1H-pyrazol-1-yl]benzenesulfonamide 
• 1443021-86-0 4-(3-(4-methoxyphenyl)-4-((phenylimino)methyl)-1H-pyrazol-1-yl)benzenesulfonamide 
• 1443021-87-1 4-(3-(4-methoxyphenyl)-4-((4-methoxyphenylimino)methyl)-1H-pyrazol-1-yl)benzenesulfonamide 
• 1443021-88-2 4-(4-((4-chlorophenylimino)methyl)-3-(4-methoxyphenyl)-1H-pyrazol-1-yl)benzenesulfonamide 
• 1443021-99-5 4-(4-(4-(4-chlorophenyl)-1-(4-fluorophenyl)-1,4-dioxobutan-2-yl)-3-(4-methoxyphenyl)-1H-pyrazol-1-yl)benzenesulfonamide 
• 1443022-00-1 4-(4-(4-(4-chlorophenyl)-1-(4-methoxyphenyl)-1,4-dioxobutan-2-yl)-3-(4-methoxyphenyl)-1H-pyrazol-1-yl)benzenesulfonamide 
• 1443022-07-8 4-(4-(5-(4-chlorophenyl)-2-(4-fluorophenyl)-1H-pyrrol-3-yl)-3-(4-methoxyphenyl)-1H-pyrazol-1-yl)benzenesulfonamide 
• 1443022-08-9 4-(4-(5-(4-chlorophenyl)-2-(4-methoxyphenyl)-1H-pyrrol-3-yl)-3-(4-methoxyphenyl)-1H-pyrazol-1-yl)benzenesulfonamide 

Relevant academic research and scientific papers

Design, synthesis of celecoxib-tolmetin drug hybrids as selective and potent COX-2 inhibitors

Three novel series of diarylpyrazole 10b-d and triarylpyrazole derivatives 11a-d &12a-d were synthesized through Vilsmier-Haack condition. The structures of prepared compounds were determined through IR, 1H NMR, 13C NMR, Mass spectral and elemental analysis. Docking of the synthesized compounds over COX-2 active site ensure their selectivity. Moreover, the target compounds were evaluated for both in vitro and in vivo inhibitory activity. All compounds were more selective for COX-2 isozyme than COX-1 isozyme and with excellent anti-inflammatory activity. Compounds 11b, 11d and 12b showed the highest anti-inflammatory activity (67.4%, 62.7%, 61.4% respectively), lower ulcerogenic liability (UI = 2.00, 2.75, 3.25 respectively) than indomethacin (UI = 14) and comparable to celecoxib (UI = 1.75) which were confirmed from the histopatholgical study.

Pyrazole-4-carboxylic Acids from Vanadium-catalyzed Chemical Transformation of Pyrazole-4-carbaldehydes

The conversion of aldehydes into carboxylic acids using oxidizing agents is a common protocol in transformation chemistry. An efficient oxidation strategy of transformation of pyrazole-4-aldehydes to the corresponding acids using vanadium catalysts in the presence of 30% H2O2 as an oxidant is described. The catalytic technology was successfully applied to a range of various 4-formylpyrazoles, and plausible mechanism is also discussed.

Pyrazolylbenzo[d]imidazoles as new potent and selective inhibitors of carbonic anhydrase isoforms hCA IX and XII

Novel pyrazolylbenzo[d]imidazole derivatives (2a-2f) were designed, synthesized and evaluated against four human carbonic anhydrase isoforms belonging to α family comprising of two cytosolic isoforms hCA I and II as well as two transmembrane tumor associated isoforms hCA IX and XII. Starting from these derivatives that showed high potency but low selectivity in favor of tumor associated isoforms hCA IX and XII, we investigated the impact of removing the sulfonamide group. Thus, analogs 3a-3f without sulfonamide moiety were synthesized and biological assay revealed a good activity as well as an excellent selectivity as inhibitors for tumor associated hCA IX and hCA XII and the same was analyzed by molecular docking studies.

Synthesis of 4-(2-substituted hydrazinyl)benzenesulfonamides and their carbonic anhydrase inhibitory effects

In this study, 4-(2-substituted hydrazinyl)benzenesulfonamides were synthesized by microwave irradiation and their chemical structures were confirmed by 1H NMR, 13CNMR, and HRMS. Ketones used were: Acetophenone (S1), 4-methylacetophe

Synthesis of novel 1,3,4-trisubstituted pyrazoles as anti-inflammatory and analgesic agents

Some novel 1,3,4-trisubstituted pyrazoles were synthesized and screened for their anti-inflammatory and analgesic activities as well as their ulcerogenic liability. They showed anti-inflammatory and analgesic activities with better GIT tolerance than the standard drug phenylbutazone. In addition, IC 50 values for 5e and 8e were recorded. Compound 5e was found to be the most active one as anti-inflammatory and analgesic agent. On the other hand, COX-1/COX-2 isozyme selectivity was also done which showed equal inhibition to both isoforms.

Synthesis and biological evaluation of some 4-functionalized-pyrazoles as antimicrobial agents

1,3-Diaryl-4-formylpyrazoles 8 bearing benzenesulfonamide moiety at position-1 were synthesized as important intermediates following Vilsmeier-Haack strategy. Aldehyde moiety of 4-formylpyrazole was then converted into carboxylic acid 9, cyano 10 and carbothioamide 11 using established procedures. Out of these 4-functionalized pyrazoles, pyrazole-4-carboxylic acids 9 and carbothioamides 11 were evaluated for their in vitro antibacterial activity against four pathogenic bacterial strains namely, Staphylococcus aureus, Bacillus subtilis (Gram-positive), Escherichia coli, Pseudomonas aeruginosa (Gram-negative), and in vitro antifungal activity against two pathogenic fungal strains namely, Aspergillus niger and Aspergillus flavus. Three tested compounds, 9e, 11b and 11f exhibited moderate antibacterial activity against Gram-positive bacteria and 9g showed moderate antifungal activity against the tested fungi. However, none of the compounds showed any activity against Gram-negative bacteria.