CAS: 27019-47-2; H-ß-Ala-Obzl.Tosoh

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CAS号104-15-4 对甲苯磺酸 | CAS号100-51-6 苯甲醇 | CAS号107-95-9 β-丙氨酸 | CAS号5910-56-5 3-[(2,2-二甲基丙酰基)氨基]丙酸

📜3-氨基丙酸苄基酯,对甲苯磺酸 以 苯甲醇 用作溶剂,化学反应 5.0H,以83%的收率获得β-丙氨酸苄酯对甲苯磺酸盐
参考文献:开发杂三芳基化合物作为亚型选择性和有效抑制 Sirt5 的新化学型
标题:开发杂三芳基化合物作为亚型选择性和有效抑制 Sirt5 的新化学型
摘要:与其他去乙酰化酶(nad +依赖性 Iii 类赖氨酸脱酰基酶)相比,Sirt5 的抑制作用尚未得到很好的研究.我们目前的工作基于最近发现的 Sirt5 抑制剂巴柳氮,这是一种经批准的药物,口服后生物利用度可忽略不计.在之前的工作中首次了解其构效关系后,我们现在能够开发出杂芳基-三芳基化合物作为一种新型化学类型的药物样,强效和亚型选择性 Sirt5 抑制剂.铅结构的不利偶氮基团以系统和全面的方式进行了修饰,使我们得到了一些开链,最重要的是,五元杂环取代物(异恶唑cg_209,三唑cg_220,吡唑cg_232) 具有非常令人鼓舞的体外活性(sirt5 上的 Ic 50在低微摩尔范围内,<10 μm).这些先进的抑制剂没有细胞毒性,并显示出非常好的药代动力学特性,这通过活细胞成像实验对线粒体的渗透性得到了证实.此外,与作为参考化合物的巴柳氮相比,计算类似物的相对游离结合亲和力的结果与体外获得的抑
Doi:10.1016/j.Ejmech.2022.114594

专利信息

专利号:US-7435791-B2
优先权日:2001-07-19
标题:Process for rapid solution synthesis of peptides
发明人：EGGEN IVO FRANCI; TEN KORTENAAR PAULUS BERNARDUS; HAASNOOT CORNELIS ALBERT GRUSON
权利人:ORGANON NV
摘要:The present invention relates to a process for rapid solution synthesis of a peptide, the process comprising repetitive cycles of steps (a)-(d):n (a) a coupling step, using an excess of an activated carboxylic component to acylate an amino component, (b) a quenching step in which a scavenger is used to remove residual activated carboxylic functions, wherein the scavenger may also be used for deprotection of the growing peptide, (c) one or more aqueous extractions and optionally, (d) a separate deprotection step, followed by one or more aqueous extractions, characterised in that the process comprises at least one step (b), referred to as step (b′), in which an amine or a thiol comprising a free anion or a latent anion is used as a scavenger of residual activated carboxylic functions. nn During the process of this invention the growing peptide need not be isolated until the final peptide sequence has been obtained. n This highly efficient process is useful for the production of oligo- and polypeptides of high purity.

专利号:US-4515920-A
优先权日:1984-04-30
标题 :Synthesis of peptides and proteins
发明人：ERICKSON BRUCE W
权利人:UNIV ROCKEFELLER
摘要:Solid phase synthesis of peptides and proteins have been improved by the use of a trifunctional segment, one functional group of which is bound to a solid support, the other two functional groups being available as substrates upon which identical proteins are synthesized.

专利号:US-2003018164-A1
优先权日:2001-07-19
标题 :Process for rapid solution synthesis of peptides

专利号:US-2004082760-A1
优先权日:2001-07-19
标 题:Process for rapid solution synthesis of peptides

专利号:US-4939261-A
优先权日:1984-06-08
标 题:N-substituted butyramide derivatives useful for treatment of conditions responsive to inhibition of enkephalinase
发明人：KSANDER GARY M
权利人:CIBA GEIGY CORP
摘要:Disclosed are compounds of the formula (I) wherein X and Y independently represent hydroxymethyl; cyano; carboxy; functionally modified carboxy selected from esterified carboxy, carbamoyl, and N-substituted carbamoyl; 5-tetrazolyl; 2-oxazolyl, 4,5-dihydro-2-oxazolyl, 2-imidazolyl or 4,5-dihydro-2-imidazolyl or any said grouping substituted by lower alkyl; R and R0 independently represent hydrogen, lower alkyl, (C3-C7)-cycloalkyl-lower alkyl, or aryl-lower alkyl in which aryl represents phenyl, pyridyl, thienyl, furyl, biphenyl or naphthyl, each unsubstituted or mono- or di-substituted by halogen, lower alkyl, hydroxy, acyloxy, lower alkoxy, trifluoromethyl or cyano; A represents straight chain (C2-C5)-alkylene; or A represents straight chain (C2-C5)-alkylene substituted by lower alkyl, by lower alkylthio-lower alkyl, by hydroxy-lower alkyl, by acyloxy-lower alkyl, by lower alkoxy-lower alkyl, by amino or acyl-amino, by amino-lower alkyl, by acylamino-lower alkyl, by (C3-C7)-cycloalkyl, by (C3-C7)-cycloalkyl-lower alkyl, by aryl or aryl-lower alkyl in which aryl represents phenyl or phenyl mono- or disubstituted by halogen, lower alkyl, lower alkoxy, hydroxy, acyloxy, trifluoromethyl or cyano; or A represents phenylene or cyclohexylene; pharmaceutically acceptable prodrug derivatives of any said compounds having a free carboxy group; pharmaceutically acceptable salts of any said compounds with a salt-forming group; methods for synthesis; pharmaceutical compositions thereof; and use thereof as enkephalinase inhibitors.

专利号:US-2006063918-A1
优先权日:2001-07-19
标 题 :Process for rapid solution synthesis of peptides