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CAS号252562-03-1 4-氨基-3-甲基苯磺酰胺 | CAS号14988-21-7 4-(乙酰基氨基)-3-甲基苯磺酰氯 | CAS号98-33-9 2-氨基甲苯-5-磺酸📜2-氨基甲苯-5-磺酸置于吡啶,盐酸,Ammonium Hydroxide,Sodium Hydroxide体系中,用 四氢呋喃,吡啶,乙醇,水 作为反应溶剂,化学反应 8.0H,反应生成 3-甲基-4-氨基苯磺酰胺
参考文献:基于吡咯的s-亚硝基谷胱甘肽还原酶抑制剂的构效关系:羧酰胺修饰
标题:基于吡咯的s-亚硝基谷胱甘肽还原酶抑制剂的构效关系:羧酰胺修饰
摘要:酶s-亚硝基谷胱甘肽还原酶(gsnor)是调节水平的乙醇脱氢酶家族(adh)的成员s-通过亚硝基硫醇分解代谢(snos)s-亚硝基谷胱甘肽(gsno).gsno和sno与许多疾病的发病机制有关,包括呼吸系统,胃肠道和心血管系统的疾病.基于吡咯的n6022最近被鉴定为有效,选择性,可逆和有效的gsnor抑制剂,目前正用于急性哮喘的临床开发中.我们在这里描述了n6022的新型基于吡咯的类似物的合成及其结构-活性关系(sar),其重点是在侧链n上的羧酰胺修饰.-苯基部分.我们已经确定了有效和新颖的gsnor抑制剂,它们在卵白蛋白(ova)诱发的哮喘小鼠模型中显示出功效.
DOI:10.1016/j.Bmcl.2012.01.047
专利信息
专利号:US-7378550-B2
优先权日:2003-03-27
标题 :Process for preparing reverse transcriptase inhibitors
发明人:MARTIN MICHAEL TOLAR
权利人:SMITHKLINE BEECHAM CORP
摘要:The present invention is directed to processes for the synthesis of intermediates useful in the preparation of non-nucleoside reverse transcriptase inhibitors.
专利号:US-7700375-B2
优先权日:2004-06-16
标 题 :Fluorescent labeling of specific protein targets in vitro and in vivo
发明人:KEILLOR JEFFREY W; MICHNICK STEPHEN W; GIROUARD STEPHANE
权利人:VALORISATION RECH LP
摘要:New methods are provided for the post-genomic era that will permit the analysis of the dynamic expression and localization of gene products in living cells. Herein we propose the development of such a method from a bioorganic approach involving organic synthesis and protein engineering. Specifically, novel compounds bearing two maleimide groups attached directly to fluorescent cores will be prepared, whose latent fluorescence is quenched until their maleimide groups undergo a specific thiol addition reaction. Complementary a-helical proteins are designed bearing two cysteine residues appropriately positioned to react with our novel fluorogens. Genetically fusing our helical probe peptides to test proteins of interest, we can selectively label the target sequence in living cells with our small synthetic fluorogenic molecules. The scope of this technique is described in the context of studying protein localization and protein-protein interactions in living cells.
专利号:EP-2402011-A1
优先权日:2004-08-25
标题:Intermediates in the synthesis of S-triazolyl alpha-mercaptoacetanildes as inhibitors of HIV reverse transcriptase
专利号:WO-9221675-A1
优先权日:1991-06-03
标题:Synthesis of optically active lactones from l-aspartic acid and intermediates thereof
专利号:EP-0643710-A1
优先权日:1991-06-03
标 题 :Synthesis of optically active lactones from l-aspartic acid and intermediates thereof
专利号:US-5322942-A
优先权日:1991-06-03
标题 :Synthesis of optically active lactones from L-aspartic acid and intermediates thereof
发明人:RAPOPORT HENRY; DENER JEFFREY M; ZHANG LIN-HAU
权利人:UNIV CALIFORNIA
摘要:Optically active lactones are described, such as an intermediate lactone having the formula ##STR1## where R and R 2 are each independently alkyl with 1 to 6 carbon atoms, cycloalkyl with 6 to 10 carbon atoms, aryl with 6 to 10 carbon atoms, or arylalkyl with 7 to 19 carbon atoms, R 4 is H or C 1-6 alkyl, and Ar is a homo- or heteroaromatic ring with 5 or 6 ring atoms being optionally substituted by C 1-6 alkyl or alkoxy groups, halogen atoms, cyano or nitro groups. Such optically active, intermediate lactones are prepared from L-aspartic acid, and can be readily converted to (+)-pilocarpine and its analogues by hydrolysis, reduction, and hydrogenation, such as to an optically active lactone having the formula ##STR2## which is (+)-pilocarpine when R is ethyl, R 4 is H, and Ar is 1-methylimidazol-5-yl.