90415-85-3Relevant academic research and scientific papers
Synthesis of: N -arylsulfonamides via Fe-promoted reaction of sulfonyl halides with nitroarenes in an aqueous medium
Jiang, Jun,Zeng, Sheng,Chen, De,Cheng, Chaozhihui,Deng, Wei,Xiang, Jiannan
supporting information, p. 5016 - 5020 (2018/07/25)
A fascinating Fe-promoted protocol for the synthesis of N-arylsulfonamides has been developed. Starting from commercially available nitroarenes and sulfonyl chlorides, moderate to excellent yields of the corresponding N-arylsulfonamides can be obtained. In particular, Fe dust serves as the sole reductant in the transformation and it can be easily performed on a large scale.
1,3,4-OXADIAZOLE SULFONAMIDE DERIVATIVE COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Paragraph 2237; 2238; 2239; 2442; 2443; 2444, (2017/02/24)
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.
Dipeptide vinyl sultams: Synthesis via the Wittig-Horner reaction and activity against papain, falcipain-2 and Plasmodium falciparum
Valente, Claudia,Guedes, Rita C.,Moreira, Rui,Iley, Jim,Gut, Jiri,Rosenthal, Philip J.
, p. 4115 - 4119 (2007/10/03)
The synthesis of phosphonate derivatives of N-phenyl- and N-benzyl-γ- and δ-sultams, and their application in the Wittig-Horner reaction with N-Boc-l-phenylalanine aldehyde to afford E- and Z-isomers, are described. These compounds were further processed to provide five dipeptide vinyl sultams, which were found to be inactive against papain at concentrations up to 50 μM. In contrast, vinyl sultams demonstrated weak activity against recombinant falcipain-2 and Plasmodium falciparum W2.
Antirheumatic
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, (2008/06/13)
A novel antirheumatic agent comprising as an active ingredient a compound of formula I: or a pharmaceutically acceptable salt or hydrate thereof.
Synthetic studies on condensed-azole derivatives. I. Synthesis and anti- asthmatic activities of ω-substituted alkylthioimidazo[1,2-b]pyridazines
Kuwahara,Kawano,Kawai,Ashida,Miyake
, p. 1505 - 1510 (2007/10/03)
A series of novel ω-substituted alkylthioimidazo[1,2-b]pyridazines was designed and synthesized in an effort to find a novel anti-asthmatic agent. The anti-asthmatic activity of these compounds was evaluated on the basis of their ability to inhibit thromboxane A2 synthetase and platelet activating factor (PAF)-induced bronchoconstriction in guinea pigs. None of these compounds significantly inhibited thromboxane A2 synthetase, though, sulfonamide derivatives potently inhibited PAF-induced bronchoconstriction. Among them, 3-(imidazo[1,2-b]pyridazin-6-yl)thiopropanesulfonamide (5) showed the most potent inhibitory effect. The anti-asthmatic effects of compound 5 in experimental models were superior to those of theophylline.
