CAS: 4392-54-5; 4-Hydrazinylbenzenesulfonamide

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CAS号63-74-1 磺胺 | CAS号14289-29-3 4-sulfamoylbenz... | CAS号98-64-6 4-氯苯磺酰胺 | CAS号21305-93-1 (E)-4-(2-benzyl... | CAS号10179-57-4 MLS-573151 | CAS号169590-42-5 塞来昔布 | CAS号170569-88-7 Mavacoxib | CAS号71203-35-5 ML141 | CAS号78794-61-3 1-(p-sulfamylph... | CAS号78794-60-2 4-[5-(4-chlorop... | CAS号42357-48-2 4-(2-methyliden...

磺胺置于盐酸,Sodium Nitrite,Tin(Ll) Chloride体系中,用 水 作为反应溶剂,化学反应 4.0H,反应生成 4-肼基苯磺酰胺
参考文献:3-Hydrazinoisatin-Based苯磺酰胺作为新型碳酸酐酶抑制剂,具有抗癌活性:合成,体外生物学评估和计算机模拟.
标题:3-Hydrazinoisatin-Based苯磺酰胺作为新型碳酸酐酶抑制剂,具有抗癌活性:合成,体外生物学评估和计算机模拟.
摘要:在这里,我们描述了设计和合成两个系列的酰胺基酰胺,其特征在于通过肼连接基连接到苯磺酰胺基团的n-未取代的(4A-C)或n-取代的(7A-O)靛红部分(作为尾巴).所有制备的磺酰胺(4A-C和7A-O)均显示出对跨膜肿瘤相关人碳酸酐酶(hca,Ec 4.2.1.1)同工型,Ix和xii的有效抑制活性,Ki范围为(8.3-65.4 Nm)和(11.9-72.9 Nm).此外,根据us-Nci方案,评估了六种磺酰胺(7E,7I,7J,7M,7N和7O)对一组六十种癌细胞系的抗增殖活性.化合物7J和7N是该测定法中最有前途的对应物,显示出对多种细胞系的广谱抗增殖活性.还,在集落形成试验中,磺酰胺7N以浓度依赖的方式显着抑制了hct-116细胞的克隆形成性.此外,进行了分子建模研究,以了解hca亚型ii和ix活性位点内目标基于伊斯汀的磺酰胺类药物(4A-C和7A-O)的合理结合相互作用和亲和力.
DOI:10.1016/j.Ejmech.2019.111768

专利信息

专利号:US-7442802-B2
优先权日:2002-06-27
标 题:Cyclooxygenase-2 selective inhibitors, compositions and methods of use
发明人：BANDARAGE UPUL K; EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; KHANAPURE SUBHASH P; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI
权利人:NITROMED INC
摘要:The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.

专利号:US-7759497-B2
优先权日:2002-05-24
标 题:Synthesis of diaryl pyrazoles
发明人：LETENDRE LEO J; MCGHEE WILLIAM D; SNODDY CYNTHIA; KLEMM GEORGE; GAUD HENRY T
权利人:PFIZER
摘要:A process for the qualitative preparation of 3-haloalkyl-1H-pyrazoles suitable for efficient, high payload commercial application.

专利号:US-2004024225-A1
优先权日:2002-05-24
标题 :Synthesis of diaryl pyrazoles

专利号:US-2007004924-A1
优先权日:2002-05-24
标题:Synthesis of diaryl pyrazoles

专利号:US-6150534-A
优先权日:1999-01-14
标题:Synthesis of 4-[5-substituted or unsubstituted phenyl)-3-substituted-1H-pyrazol-1-yl]benzenesulfonamides

专利号:US-6232472-B1
优先权日:1999-01-14
标题:Synthesis of 4-[(5-substituted phenyl)-3-substituted-1H-pyrazol-1-yl]benzenesulfonamide
发明人：O'SHEA PAUL; WANG XIN; TILLYER RICHARD D; CLAS SOPHIE-DOROTHEE; DALTON CHAD
权利人:MERCK FROSST CANADA INC
摘要:This invention encompasses a novel process for synthesizing the compound represented by formula I:These compounds are useful as non-steroidal anti-inflammatory agents.