CAS: 144665-07-6; Lubeluzole

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N-Methyl-N-(Piperidin-4-yl)-1,3-Benzothiazol-2-Amine 104605-42-7
Ethyl 4-[1,3-Benzothiazol-2-Yl(Methyl)Amino]Piperidine-1-Carboxylate 139051-64-2

📜2-氯苯并噻唑置于氢溴酸,溶剂黄146,三乙胺,Ytterbium(III) Triflate体系中,用 二氯甲烷,乙二醇 用作溶剂,化学反应 2.08H,反应生成(2S)-1-[4-(1,3-苯并噻唑-2-基-甲基氨基)哌啶-1-基]-3-(3,4-二氟苯氧基)丙-2-醇
参考文献:化学增敏剂lubeluzole结合钙调蛋白并抑制ca 2+ /钙调蛋白依赖性激酶ii
标题:化学增敏剂lubeluzole结合钙调蛋白并抑制ca 2+ /钙调蛋白依赖性激酶ii
摘要:开发了一种亲和毛细管电泳(ace)方法来估计牛脑钙调蛋白(cam)与非肽配体之间的表观解离常数.该方法经过验证,可重现许多众所周知的cam配体的解离常数.特别地,通过改进的合成方法临时合成了有效的拮抗剂125-C9 .Ace方法已成功应用于验证cam对lubeluzole的亲和力,Lubeluzole是一种最近被证明可用于增强抗癌药活性的著名神经保护剂.鲁贝鲁唑略低于有力超过125-C9(ķ D 分别= 2.9+/-0.7和0.47+/-0.06μm,)并显示的ca 2+ /钙调蛋白依赖性激酶ii(camkii的)抑制(ic 50 = 40+/-1μm).通过对接研究,基于几种三氟拉嗪-Cam配合物的x射线晶体结构,探索了lubeluzole与cam的可能结合方式.发现估计的解离常数与实验值非常好吻合,并突出了主要的氨基酸残基和相互作用,促进了复合物的形成.讨论了干扰ca 2+途径可能有助于先前观测到的
Doi:10.1016/j.Ejmech.2016.03.045

专利信息

专利号:US-2014315720-A1
优先权日:2012-10-24
标 题 :Polysaccharide ester microspheres and methods and articles relating thereto
发明人：FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY
权利人:CELANESE ACETATE LLC
摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.