New stereoselective titanium reductive amination synthesis of 3-amino and polyaminosterol derivatives possessing antimicrobial activities.

Salmi C; Loncle C; Vidal N; Letourneux Y; Brunel JM

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New stereoselective titanium reductive amination synthesis of 3-amino and polyaminosterol derivatives possessing antimicrobial activities.

机译：具有抗菌活性的3-氨基和聚氨基甾醇衍生物的新型立体选择性钛还原胺化合成。

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摘要

A series of 3-amino and polyaminosterol analogues of squalamine and trodusquemine were synthesized involving a new stereoselective titanium reductive amination reaction in high chemical yields of up to 95% in numerous cases. These derivatives were evaluated for their in vitro antimicrobial properties against human pathogens. Activity was highly dependent on the different compounds' structures involved and best results have been obtained with aminosterol derivatives 4b, 4e and 6i exhibiting activities against yeasts, Gram positive and Gram negative bacteria at average concentrations of 6.25-12.5 microg/mL.

机译：合成了一系列的角鲨胺和曲妥斯克明的3-氨基和聚氨基甾醇类似物，涉及一种新的立体选择性钛还原胺化反应，在许多情况下化学产率高达95％。对这些衍生物的体外抗人类病原体抗菌性能进行了评估。活性高度依赖于所涉及的不同化合物的结构，氨基固醇衍生物4b，4e和6i在平均浓度为6.25-12.5 microg / mL时对酵母，革兰氏阳性和革兰氏阴性细菌表现出活性，从而获得了最佳结果。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2008年第3期|共8页
作者
Salmi C; Loncle C; Vidal N; Letourneux Y; Brunel JM;
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原文格式 PDF
正文语种 eng
中图分类医药、卫生;劳动卫生;
关键词
derivatives; Titanium; Amination; New; Endurance of activity; 钛; 胺化作用;

机译：derivatives;Titanium;Amination;New;Endurance of activity;钛;胺化作用;

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1. New stereoselective titanium reductive amination synthesis of 3-amino and polyaminosterol derivatives possessing antimicrobial activities. [J] . Salmi C, Loncle C, Vidal N, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2008,第3期

机译：具有抗菌活性的3-氨基和聚氨基甾醇衍生物的新型立体选择性钛还原胺化合成。
2. Stereoselective synthesis of 3,7-diarylaminocholestanes by titanium-mediated reductive amination [J] . Md. Wasi Ahmad, Hong-Seok Kim Steroids: An International Journal . 2014,第Null期

机译：钛介导的还原胺化立体选择性合成3,7-二芳基氨基胆甾烷
3. Stereoselective Synthesis of Hydroxy Diamino Acid Derivatives and the Caprolactam Unit of Bengamide A through Organocatalytic -Hydroxylation and Reductive Amination of Aldehydes [J] . Philip Anijamol T., Raju Eerlapally, Ramapanicker Ramesh European journal of organic chemistry . 2016,第33期

机译：通过醛的有机催化-羟基氧化和还原胺化立体选择性合成羟基二氨基酸衍生物和Bengamide A的己内酰胺单元
4. Reductive Cross-amination between Aniline or Nitroarene Derivatives and Alkylamines Catalyzed by Polysilane-immobilized Metal Nanoparticles [C] . Aya SUZUKI, Hiroyuki MIYAMURA, Shu KOBAYASHI 日本化学会春季年会講演予稿集 . 2018

机译：通过聚硅烷固定金属纳米颗粒催化的苯胺或硝基芳衍生物和烷基胺之间的还原交叉胺化
5. Asymmetric synthesis of 1,3-amino alcohols and tropinone derivatives from enantiopure sulfinimines. [D] . Gaspari, Paul. 2011

机译：从对映体纯的亚磺酸亚胺不对称合成1,3-氨基醇和肌钙蛋白衍生物。
6. Stereoselective Radical Amination of Electron-Deficient C(sp3)–H Bonds by Co(II)-Based Metalloradical Catalysis: Direct Synthesis of α-Amino Acid Derivatives via α-C–H Amination [O] . Hongjian Lu, Yang Hu, Huiling Jiang, -1

机译：缺电子C（sp3）-H债券的立体选择性自由基胺化由钴（II）-Based metalloradical催化：通过α-C-H的胺化α氨基酸衍生物的直接合成
7. Synthesis of Novel Inhibitors of IdeS, a Bacterial Cysteine Protease Including Studies of Stereoselective Reductive Aminations [O] . Berggren Kristina 2011

机译：新型抑制剂Ides的合成，一种细菌半胱氨酸蛋白酶，包括立体选择性还原胺化的研究

New stereoselective titanium reductive amination synthesis of 3-amino and polyaminosterol derivatives possessing antimicrobial activities.

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