Synthesis and extended activity of triazole-containing macrocyclic protease inhibitors

Pehere A.D.; Pietsch M.; Gütschow M.; Neilsen P.M.; Pedersen D.S.; Nguyen S.; Zvarec O.; Sykes M.J.; Callen D.F.; Abell A.D.

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Synthesis and extended activity of triazole-containing macrocyclic protease inhibitors

机译：含三唑的大环蛋白酶抑制剂的合成及扩展活性

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Peptide-derived protease inhibitors are an important class of compounds with the potential to treat a wide range of diseases. Herein, we describe the synthesis of a series of triazole- containing macrocyclic protease inhibitors pre-organized into a b-strand conformation and an evaluation of their activity against a panel of proteases. Acyclic azidoalkyne-based aldehydes are also evaluated for comparison. The macrocyclic peptidomimetics showed considerable activity towards calpain II, cathepsin L and S, and the 20S proteasome chymotrypsin-like activity. Some of the first examples of highly potent macrocyclic inhibitors of cathepsin S were identified. These adopt a well-defined b-strand geometry as shown by NMR spectroscopy, X-ray analysis, and molecular docking studies.

机译：肽衍生的蛋白酶抑制剂是一类重要的化合物，具有治疗多种疾病的潜力。本文中，我们描述了一系列预组织为b链构象的含三唑的大环蛋白酶抑制剂的合成及其对一组蛋白酶的活性评估。还评估了基于无环叠氮炔的醛以进行比较。大环肽模拟物对钙蛋白酶II，组织蛋白酶L和S以及20S蛋白酶体胰凝乳蛋白酶样活性表现出相当大的活性。鉴定了组织蛋白酶S的强效大环抑制剂的一些第一个实例。它们采用了明确定义的b链几何结构，如NMR光谱，X射线分析和分子对接研究所示。

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《Chemistry: A European journal》 |2013年第24期|共7页
作者
Pehere A.D.; Pietsch M.; Gütschow M.; Neilsen P.M.; Pedersen D.S.; Nguyen S.; Zvarec O.; Sykes M.J.; Callen D.F.; Abell A.D.;
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正文语种 eng
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click chemistry; macrocycles; NMR spectroscopy; peptidomimetics; protease inhibitors;

机译：点击化学;大环化合物;NMR光谱;拟肽;蛋白酶抑制剂;

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1. Synthesis and extended activity of triazole-containing macrocyclic protease inhibitors [J] . Pehere A.D., Pietsch M., Gütschow M., Chemistry: A European journal . 2013,第24期

机译：含三唑的大环蛋白酶抑制剂的合成及扩展活性
2. Synthesis, antiviral activity, and conformational studies of a P3 aza-peptide analog of a potent macrocyclic tripeptide HCV protease inhibitor. [J] . Randolph JT, Zhang X, Huang PP, Bioorganic and Medicinal Chemistry Letters . 2008,第8期

机译：高效大环三肽HCV蛋白酶抑制剂P3 AZA肽类似物的合成，抗病毒活性和构象研究。
3. Synthesis and biological activity of macrocyclic inhibitors of hepatitis C virus (HCV) NS3 protease. [J] . Chen KX, Njoroge FG, Prongay A, Bioorganic and Medicinal Chemistry Letters . 2005,第20期

机译：丙型肝炎病毒（HCV）NS3蛋白酶大环抑制剂的合成和生物学活性。
4. Synthesis and Structure-Activity Relationship of Marinostatin, An Ester-Linked Serine Protease Inhibitor [C] . Misako Taichi, Toshimasa Yamazaki, Tadashi Teshima, Chinese international peptide symposium . 2011

机译：Marinostatin的合成与结构 - 活性关系，酯连接丝氨酸蛋白酶抑制剂
5. Design and synthesis of core structural intermediates for novel HIV-1 protease inhibitors and synthesis, biological activity and molecular modeling of novel 20S proteasome inhibitors. [D] . Avancha, Kiran Kumar Venkata Raja. 2006

机译：新型HIV-1蛋白酶抑制剂的核心结构中间体的设计与合成，新型20S蛋白酶体抑制剂的合成，生物学活性和分子建模。
6. Structure-Based Design and Synthesis of Triazole-based Macrocyclic Inhibitors of Norovirus Protease: Structural Biochemical Spectroscopic and Antiviral Studies [O] . Pathum M. Weerawarna, Yunjeong Kim, Anushka C. Galasiti Kankanamalage, -1

机译：基于三唑的诺如病毒蛋白酶大环抑制剂的结构设计与合成：结构生化光谱和抗病毒研究
7. Design, synthesis, and evaluation of a novel series of macrocyclic inhibitors of norovirus 3CL protease [O] . Damalanka, Vishnu C., Kim, Yunjeong, Kankanamalage, Anushka C. Galasiti, 2017

机译：新型诺如病毒3CL蛋白酶大环抑制剂系列的设计，合成和评估

Synthesis and extended activity of triazole-containing macrocyclic protease inhibitors

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