7117-21-7

Upstream product

• 56146-84-0 ethyl phenylamino-sulphonylacetate 
• 62-53-3 aniline 
• 13229-32-8 methyl 2‐(phenylsulfamoyl)acetate 

Downstream Products

• 56146-79-3 N-(2,4-Dinitrophenyl)-aminosulfonylessigsaeure 
• 13719-47-6 (E)-N,2-diphenylethene-1-sulfonamide 
• 1427286-04-1 4-phenyl-3-phenylaminosulfonylpyrrole 
• 1612842-13-3 3-chloro-4-(2-fluoro-4-(2-(N-phenylsulfamoyl)acetamido)phenoxy)picolinamide 
• 1612842-19-9 N-(4-((2-amino-3-chloropyridin-4-yl)oxy)-3-fluorophenyl)-2-(N-phenylsulfamoyl)acetamide 
• 1246440-71-0 2-phenylaminosulfonylmethyl-5-phenyl-1,3,4-oxadiazole 
• 56146-80-6 trans-2',4'-Dinitrostyrol-β-sulfonylanilid 
• 78374-44-4 (E)-2-(5-Nitro-thiophen-2-yl)-ethenesulfonic acid phenylamide 
• 78374-38-6 2-<(5-nitro-2-furyl)vinyl>sulphonanilide 
• 78374-26-2 (E)-2-(5-Nitro-thiophen-2-yl)-ethenesulfonic acid acetyl-phenyl-amide 
• 78374-20-6 N-acetyl-2-<(5-nitro-2-furyl)vinyl>sulphonanilide 

Relevant academic research and scientific papers

Discovery of a series of ester-substituted NLRP3 inflammasome inhibitors

The NLRP3 inflammasome is a component of the innate immune system involved in the production of proinflammatory cytokines. Aberrant activation by a wide range of exogenous and endogenous signals can lead to chronic, low-grade inflammation. It has attracted a great deal of interest as a drug target due to the association with diseases of large unmet medical need such as Alzheimer's disease, Parkinson's disease, arthritis, and cancer. To date, no drugs specifically targeting inhibition of the NLRP3 inflammasome have been approved. In this work, we used the known NLRP3 inflammasome inhibitor CP-456,773 (aka CRID3 or MCC 950) as our starting point and undertook a Structure-Activity Relationship (SAR) analysis and subsequent scaffold-hopping exercise. This resulted in the rational design of a series of novel ester-substituted urea compounds that are highly potent and selective NLRP3 inflammasome inhibitors, as exemplified by compounds 44 and 45. It is hypothesized that the ester moiety acts as a highly permeable delivery vehicle and is subsequently hydrolyzed to the carboxylic acid active species by carboxylesterase enzymes. These molecules are greatly differentiated from the state-of-the-art and offer potential in the treatment of NLRP3-driven diseases, particularly where tissue penetration is required.

Discovery of novel type II c-Met inhibitors based on BMS-777607

Twenty-two new analogs based on the structure of BMS-777607 were designed, synthesized, and evaluated to determine their biological activities. Compounds bearing a cyclic sulfonamide or α-chloropiperidone scaffold exhibited good activity, which may provid

Design, synthesis, and biological evaluation of (E)-N-Aryl-2- arylethenesulfonamide analogues as potent and orally bioavailable microtubule-targeted anticancer agents

A series of novel (E)-N-aryl-2-arylethenesulfonamides (6) were synthesized and evaluated for their anticancer activity. Some of the compounds in this series showed potent cytotoxicity against a wide spectrum of cancer cell-lines (IC50 values ranging from 5 to 10 nM) including all drug resistant cell-lines. Nude mice xenograft assays with compound (E)-N-(3-amino-4- methoxyphenyl)-2-(2′,4′,6′-trimethoxyphenyl)ethenesulfonamide (6t) showed dramatic reduction in tumor size, indicating their in vivo potential as anticancer agents. A preliminary drug development study with compound 6t is predicted to have increased blood-brain barrier permeability relative to many clinically used antimitotic agents. Mechanistic studies indicate that 6t and some other analogues disrupted microtubule formation, formation of mitotic spindles, and arrest of cells in mitotic phase. Compound 6t inhibited purified tubulin polymerization in vitro and in vivo and circumvented drug resistance mediated by P-glycoprotein. Compound 6t specifically competed with colchicine binding to tubulin and with similar avidity as podophylltoxin, indicating its binding site on tubulin.

Synthesis and bioassay of aminosulfonyl-1,3,4-oxadiazoles and their interconversion to 1,3,4-thiadiazoles

A new class of oxadiazoles is prepared by treating aminosulfonylacetic acids with different carboxylic acid hydrazides. Interconversion of oxadiazoles to thiadiazoles is carried out with thiourea. The compounds are screened for antimicrobial and antioxidant activities.

IL-8 receptor antagonists

The present invention involves certain 8-ureido and 8-thioureido, 1,2-benzothiazines, 1,2,4-benzothioxazines and 1,2,4-benzothiodiazines useful in the treatment of disease states mediated by the chemokine, Interleukin-8.

Synthese, complexation et mecanisme d'hydrolyse de sulfamoylacetates d'alkyle, inhibiteurs de l'alcool coniferylique deshydrogenase

Alkyl sulfamoylacetates and their derivatives, inhibitors of coniferylalcohol deshydrogenase (CADH), were prepared with 40-80percent yield either by oxidation of the corresponding alkyl sulfinamoylacetates or by reaction of functionnalised sulfonyl chlorides with amines.The kinetics of hydrolysis of methyl N-phenyl sulfamoylacetate 7 leads us to propose a BAC2 mechanism of slow hydroxide ion attack at the carbonyl carbon atom.It is different from that proposed for the basic hydrolysis of the alkylsulfinamoylacetates.Sulfamoylesters do not complex ZnBr2 in CHCl3 medium at the contrary of the sulfinamoylesters.The sites and the complexation constants have been found by 1H NMR, using shift reagent .The reaction of ZnBr2/THF with the tert-butyl esters of the titled compounds leads to the formation of the Zn2+ salt of the acid.These results have been correlated with the differences of biologic activity of these compounds during the inactivation of CADH.

Synthesis and Biological Activity of Some New 2--N-arylsulphonamides and 1-sulphonyl Heterocycles

Several new 2--N-arylsulphonamides (10-12) and 1-2-(5-nitro-2-furyl- and 5-nitro-2-thienyl)vinyl sulphonyl heterocycles (13-16) have been synthesized and evaluated for various biological activities.Three com