Facing the gem-dialkyl effect in enzyme inhibitor design: Preparation of homocycloleucine-based azadipeptide nitriles

Frizler M.; Lohr F.; Lülsdorff M.; Gütschow M.

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Facing the gem-dialkyl effect in enzyme inhibitor design: Preparation of homocycloleucine-based azadipeptide nitriles

机译：面对酶抑制剂设计中的宝石二烷基效应：基于同环亮氨酸的氮杂二肽腈的制备

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A tough nut to crack: In contrast to azadipeptide nitriles containing a P2 leucine residue, the synthesis of the corresponding homocycloleucine-based inhibitors was more difficu possibly due to the gem-dialkyl effect. A synthetic route to the first homocycloleucine-derived azadipeptide nitriles as selective and highly potent cathepsin K inhibitors is presented (see scheme).

机译：一个难以破解的坚果：与含有P2亮氨酸残基的氮杂肽腈相比，相应的基于同环亮氨酸的抑制剂的合成更加困难。可能是由于宝石二烷基效应。提出了合成第一个由高环亮氨酸衍生的氮杂二肽腈作为选择性和高效组织蛋白酶K抑制剂的合成途径（参见方案）。

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《Chemistry: A European journal》 |2011年第41期|共5页
作者
Frizler M.; Lohr F.; Lülsdorff M.; Gütschow M.;
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原文格式 PDF
正文语种 eng
中图分类应用化学;
关键词
azapeptides; cathepsin K; drug design; enzymes; inhibitors;

机译：氮杂肽;蛋白酶K;药物设计;酶;抑制剂;

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1. Facing the gem-dialkyl effect in enzyme inhibitor design: Preparation of homocycloleucine-based azadipeptide nitriles [J] . Frizler M., Lohr F., Lülsdorff M., Chemistry: A European journal . 2011,第41期

机译：面对酶抑制剂设计中的宝石二烷基效应：基于同环亮氨酸的氮杂二肽腈的制备
2. Highly selective azadipeptide nitrile inhibitors for cathepsin K: design,synthesis and activity assayst [J] . Xing-Feng Ren, Hong-Wei Li, Xuexun Fang, Organic & biomolecular chemistry . 2013,第7期

机译：组织蛋白酶K的高选择性氮杂二肽腈抑制剂：设计，合成和活性测定
3. Design, synthesis and biological evaluation of potent azadipeptide nitrile inhibitors and activity-based probes as promising anti-Trypanosoma brucei agents [J] . Yang P.-Y., Wang M., Li L., Chemistry: A European journal . 2012,第21期

机译：有效的氮杂二肽腈抑制剂和基于活性的探针作为有希望的抗布鲁氏锥虫药物的设计，合成和生物学评估
4. Cyclohexadiene-trans-diols:Preparation with Recombinant Cells of E.coli and Application in the Chemistry of New Enzyme Inhibitors [C] . Franke.D.Lorbach International meeting on chemical engineering and biotechnology;AchemAsia 2001 . 2001

机译：环己二烯反式-二醇：大肠杆菌重组细胞的制备及其在新型酶抑制剂中的应用
5. Rational Design of Novel Antibiotics: Enzyme Inhibitors Exploiting Halogen Bonding =Rational Design of Novel Antibiotics: Enzyme Inhibitors Exploiting Halogen Bonding [D] . DePaola, Taran S. 2020

机译：新型抗生素的理性设计：酶抑制剂利用卤素键合=新型抗生素的合理设计：酶抑制剂利用卤素键合
6. Antimalarial Activity of Azadipeptide Nitriles [O] . Reik Löser, Jiri Gut, Philip J. Rosenthal, -1

机译：硫代肽腈的抗疟疾活性
7. Antimalarial activity of azadipeptide nitriles [O] . Löser, Reik, Gut, Jiri, J. Rosenthal, Philip, 2010

机译：氮杂二肽腈的抗疟活性

Facing the gem-dialkyl effect in enzyme inhibitor design: Preparation of homocycloleucine-based azadipeptide nitriles

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