13229-32-8

Upstream product

• 67-56-1 methanol 
• 7117-21-7 2‐(phenylsulfamoyl)acetatic acid 
• 56146-83-9 chlorosulfonyl-acetic acid methyl ester 
• 62-53-3 aniline 
• 29508-16-5 sodium 2-methoxy-2-oxoethane-1-sulfonate 

Downstream Products

• 1606125-04-5 C₁₉H₁₉N₅O₅S₂ 
• 1606125-01-2 C₁₉H₁₇N₃O₅S₃ 
• 1606125-49-8 C₁₉H₁₉N₇O₄S₂ 
• 1606125-46-5 C₁₉H₁₇N₅O₄S₃ 
• 1606125-43-2 C₁₉H₁₇N₅O₅S₂ 
• 1606125-31-8 C₂₀H₁₉N₇O₅S₂ 
• 1606125-28-3 C₂₀H₁₇N₅O₅S₃ 
• 1606125-25-0 C₂₀H₁₇N₅O₆S₂ 
• 1606125-40-9 C₁₉H₂₁N₇O₄S₂ 
• 1606125-37-4 C₁₉H₁₉N₅O₄S₃ 
• 1606125-34-1 C₁₉H₁₉N₅O₅S₂ 
• 1606124-98-4 C₁₉H₁₇N₃O₆S₂ 
• 1606125-22-7 C₂₀H₂₁N₇O₅S₂ 
• 1606125-19-2 C₂₀H₁₉N₅O₅S₃ 

Relevant academic research and scientific papers

Coumarin sulfonamides and amides derivatives: Design, synthesis, and antitumor activity in vitro

Coumarins possesses immeasurable antitumor potential with minimum side effects depending on the substitutions on the basic nucleus, which exhibits great prospects for antitumor drug development. In an attempt to develop novel antitumor candidates, a series of coumarin sulfonamides and amides derivatives were designed and synthetized. The majority of these derivatives showed good cytotoxic activity against MDA-MB-231 and KB cell lines, among which compound 9c was the most potent against MDA-MB-231 cells, with IC50 value of 9.33 μM, comparable to 5-fluorouracil. Further investigation revealed that compound 9c had versatile properties against tumors, including inhibition of cell migration and invasion as well as inducing apoptosis. Reactive oxygen species (ROS) assay and western blotting analysis suggested that compound 9c promoted cancer cell apoptosis by increasing ROS levels and upregulating the expression of caspase-3 in MDA-MB-231 cells. These results indicated that compound 9c could be promising lead compound for further antitumor drug research.

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.

Synthesis, characterization and antioxidant activity of bis (arylsulfonylmethyl/arylaminosulfonylmethylazolyl) pyridines

A new class of bis(arylsulfonylmethylazolyl)pyridines and bis(arylaminosulfonylmethyl-azolyl)pyridines were synthesized from the synthetic intermediates methyl arylsulfonylacetic acid hydrazide and methyl arylaminosulfonylacetic acid hydrazide adopting a green methodology-ultrasonication. All the synthesized compounds were resulted in higher yield and in shorter reaction times. The spectral parameters such as IR, 1H NMR, 13C NMR, mass and microanalyzes were used to determine the structures of all the synthesized compounds and were assayed for antioxidant activity. The bis(arylaminosulfonylmethylazolyl)pyridines showed higher radical scavenging activity than the bis(arylsulfonylmethylazolyl)pyridines. Besides, unsubstituted, and methyl substituted compounds exhibited greater activity. Among all the tested compounds 8b and 11b were identified as potential antioxidants.

1,3,4-OXADIAZOLE SULFONAMIDE DERIVATIVE COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

The present invention relates to novel compounds represented by the formula I having histone deacetylase 6 (HDAC6) inhibitory activity, stereoisomers thereof or pharmaceutically acceptable salts thereof, the use thereof for the preparation of therapeutic medicaments, pharmaceutical compositions containing the same, a method for treating diseases using the composition, and methods for preparing the novel compounds. (I) The novel compounds, stereoisomers thereof or pharmaceutically acceptable salts thereof according to the present invention have histone deacetylase (HDAC) inhibitory activity and are effective for the prevention or treatment of HDAC6-mediated diseases.

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.

Synthesis of sultams by cycloalkylation of (alkoxycarbonylmethane) sulfonanilides

(Methoxycarbonylmethane)sulfonanilides are alkylated by α, ω-dihaloalkanes in K2CO3-DMF with the formation of sultams. A high sensitivity has been detected for the reaction rate on the electronic effect of substituents in the aromatic nucleus, although substituents in the ortho position do not obstruct the reaction and in the case of 2,6-disubstituted derivatives the reaction rate and sultam yield were maximal. Tertiary sulfonamides form derivatives of 1-sulfamoylcyclopropanecarboxylic acid under these conditions.

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.

Fungicidal, miticidal and ovicidal alkoxycarbonylalkyl-substituted and carbamylalkyl-substituted N-haloalkylthiosulfonamides

Fungi, mites and mite eggs are killed by applying thereto sulfonamides of the formula STR1 wherein R and R1 individually are alkyl, cycloalkyl, aryl, carbamylalkyl, or alkoxycarbonylalkyl and R2 is haloalkyl, with the proviso that one R or R1 group is carbamylalkyl or alkoxycarbonylalkyl.