α-Methylene tetrazole-based peptidomimetics: synthesis and inhibition of HIV protease

Barnaby C. H. May and Andrew D. Abell

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α-Methylene tetrazole-based peptidomimetics: synthesis and inhibition of HIV protease

机译：基于α-亚甲基四唑的拟肽：合成和抑制HIV蛋白酶

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An α-methylene tetrazole-based dipeptidomimetic (11) has been prepared as a constrained and non-hydrolysablencore for incorporation into peptides. A single crystal X-ray structure determination revealed that its solid-statenconformation closely resembles that of the isosteric core of JG-365 bound to HIV protease. The α-methylenentetrazole isosteric unit was then incorporated into a number of peptide sequences and the resulting compoundsn6–8 were assayed against HIV protease. The assay results suggest that the longer the C-terminal substitutionnthe greater the potency, a result that reflects the interplay of the geometry of the tetrazole isostere and thenC-terminal substituent.

机译：已经制备了一种基于α-亚甲基四唑的二肽模拟物（11），作为一种受约束且不可水解的核，可以掺入肽中。单晶X射线结构测定表明，其固态构象与结合到HIV蛋白酶的JG-365的等构核非常相似。然后，将α-亚甲基四唑等位单元并入许多肽序列中，并对所得化合物n6-8进行HIV蛋白酶检测。分析结果表明，C末端取代的时间越长，效力越强，该结果反映了四唑等排物和C末端取代基的几何结构相互影响。

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《Journal of the Chemical Society, Perkin Transactions 1》 |2002年第2期|p.172-178|共7页
作者
Barnaby C. H. May and Andrew D. Abell;
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a Department of Chemistry, University of Canterbury, Private Bag 4800, Christchurch,New Zealand. E-mail: a.abell@chem.canterbury.ac.nzb Department of Cellular and Molecular Pharmacology, University of California San Francisco,San Francisco, California 94143-0450, USA. E-mail: alchemi@itsa.ucsf.edu;

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1. alpha-Methylene tetrazole-based peptidomimetics: synthesis and inhibition of HIV protease [J] . May BCH., Abell AD. Journal of the Chemical Society, Perkin Transactions 1 . 2002,第2期

机译：基于α-亚甲基四唑的拟肽：合成和抑制HIV蛋白酶
2. Hydroxyethylamine Isostere of an HIV-1 Protease Inhibitor Prefers Its Amine to the Hydroxy Group in Binding to Catalytic Aspartates. A Synchrotron Study of HIV-1 Protease in Complex with a Peptidomimetic Inhibitor [J] . Jan Dohnalek, Jindrich Hasek, Jarmila Duskova, Journal of Medicinal Chemistry . 2002,第7期

机译：HIV-1蛋白酶抑制剂的羟乙基胺等排物在与催化天冬氨酸结合时更喜欢其胺基而不是羟基。与拟肽抑制剂复合的HIV-1蛋白酶的同步加速器研究。
3. Diversity‐Oriented Synthesis of Diol‐Based Peptidomimetics as Potential HIV Protease Inhibitors and Antitumor Agents [J] . Vadhadiya Paresh M., Jean Marc‐Alexandre, Bouzriba Chahrazed, Chembiochem: A European journal of chemical biology . 2018,第16期

机译：基于二醇的肽模拟物的分量为潜在的HIV蛋白酶抑制剂和抗肿瘤剂
4. Prodrug forms of peptidomimetic HIV protease inhibitors using intramolecular cyclization reaction [C] . Yoshiaki Kiso, Hikaru Matsumoto, Tomonori Hamawaki, the International Peptide Symposium . 2001

机译：使用分子内环化反应的肽瘤HIV蛋白酶抑制剂的前药形式
5. The roles of multiple transporters in the intestinal abosrption of saquinavir, a peptidomimetic HIV protease inhibitor. [D] . Williams, Gregory Charles. 2002

机译：多种转运蛋白在沙奎那韦（一种拟肽的HIV蛋白酶抑制剂）的肠道吸收中的作用。
6. Synthesis of Bis-Glyoxylamide Peptidomimetics Derived from Bis-N-acetylisatins Linked at C5 by a Methylene or Oxygen Bridge [O] . Venty Suryanti, Ruonan Zhang, Vina Aldilla, 2019

机译：衍生自由亚甲基或氧桥在C5连接的Bis-N-乙酰基靛红衍生的Bis-乙二醛酰胺拟肽
7. Diversity-Oriented Synthesis of Diol-Based Peptidomimetics as Potential HIV Protease Inhibitors and Antitumor Agents [O] . Paresh M. Vadhadiya, Marc-Alexandre Jean, Chahrazed Bouzriba, 2018

机译：基于二醇的肽模拟物的分量为潜在的HIV蛋白酶抑制剂和抗肿瘤剂

α-Methylene tetrazole-based peptidomimetics: synthesis and inhibition of HIV protease

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