10305-42-7Relevant articles and documents
Sulfonamides 18 β - glycyrrhetinic acid derivatives and preparation method and application thereof
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Paragraph 0087; 0095; 0097, (2021/11/19)
The invention provides a sulfonamides 18 β - glycyrrhetinic acid derivative as well as a preparation method and application thereof. Belong to medicine technical field. To the invention, the series of derivatives of 18 β - glycyrrhetinic acid modified by sulfonamide groups is designed and synthesized. By introducing an active sulfonamide group, the water solubility and the bioavailability of the compound can be significantly improved to improve the antitumor activity of the related derivative. Experiments prove that the compound 6a has excellent cytotoxic activity for 3 human cancer cells (MCF - 7, A549, HEPG2), is far higher than the parent drug GA, and the activity of the compound 6a in comparison with the positive control anti-cancer drug gefitinib is remarkably improved. The compound is expected to be a prodrug for replacing gefitinib. The drug resistance of the cancer patients to gefitinib can be solved. Thus, the utility model has good practical application value.
For horse west for tanzania intermediate preparation method (by machine translation)
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Paragraph 0026; 0027; 0028; 0033-0035; 0040-0042; 0047-0049, (2017/10/27)
The invention discloses a method for horse west for tanzania intermediate is third amidogen preparation of sulfonamides method, including: to propylamine and chloride as the starting material, triethylamine as acid-binding agent, through the two-step reaction is third amidogen sulfonamide crude product, after treatment distillation to obtain the states the propylamine base sulfonamide. Preparation method of this invention uses cheap and easily available raw materials, each step the reaction operation is simple, the reaction step and short reaction time, easy purification, high yield, low cost, and is suitable for industrial mass production. (by machine translation)
2,1,3-Benzothiadiazine derivatives: Synthesis and screening versus PDE4 enzyme
Tait, Annalisa,Luppi, Amedeo,Avallone, Rossella,Baraldi, Mario
, p. 653 - 663 (2007/10/03)
A series of N-1,3 disubstituted 2,1,3-benzothiadiazine derivatives (BTDs) were synthesized and evaluated for their inhibitory activity versus enzymatic isoform PDE4 extracted from U937 cell line. Some of the tested compounds showed a high PDE4 inhibitory activity at 100:μM and the IC50 value of the most interesting terms were evaluated. The structure-activity relationships of these compounds showed that the 3,5-di-tert-butyl-4-hydroxybenzyl moiety at N-1 position is important to obtain activity at micromolar level as previously reported. For the same compounds the antioxidant activity were evaluated highlighting 14 as the most significative one. The introduction of other bulky substituents in N-1 position is detrimental.
Synthesis, biological evaluation and molecular modelling studies on benzothiadiazine derivatives as PDE4 selective inhibitors
Tait, Annalisa,Luppi, Amedeo,Hatzelmann, Armin,Fossa, Paola,Mosti, Luisa
, p. 1393 - 1402 (2007/10/03)
A series of 2,1,3- and 1,2,4-benzothiadiazine derivatives (BTDs) were synthesized and evaluated for their inhibitory activity versus enzymatic isoforms PDE3, PDE4 and PDE7. The compounds characterized by the 3,5-di-tert-butyl-4-hydroxybenzyl moiety at N1
N-pyrazinecarbonyl-N'-substituted-sulfamoylguanidine and processes for preparing same
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, (2008/06/13)
The case involves novel N-pyrazinecarbonyl-N'-substituted-sulfamoylguanidine and processes for preparing same. The N-pyrazinecarbonyl-N'-substituted-sulfamoylguanidines are excellent eukalemic agents possessing diuretic and natriuretic properties.
Production of sulfamic acid halides
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, (2008/06/13)
The production of sulfamic acid halides by reaction of sulfamic acids with acid halides, and the new sulfamic acid halides. The products are starting materials for the production of plant protection agents, dyes and pharmaceuticals.