Synthesis and biological activity of new glycyrrhizic acid conjugates with amino acids and dipeptides

机译：新型含氨基酸和二肽的甘草酸缀合物的合成及生物活性

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New glycyrrhizic acid (GA) conjugates were synthesized with the use of -butyl esters of amino acids or benzyl esters of dipeptides; they contained two residues of -amino acids (Met, Phe, Pro, and Ile or dipeptides Gly-Leu and Gly-Phe). Activation of GA carboxy groups was carried out with the help of -hydroxysuccinimide, -dicyclohexylcarbodiimide, or -hydroxybenzotriazole with dicyclohexylcarbodiimide. A proline-containing GA derivative is a low-toxic substance; it raises the level of agglutinins by 3.7 times in the blood of mice and 3 times that of hemolysins compared with the control. Dipeptide GA derivatives possess an expressed anti-HIV-1 activity in cultures of MT-4 cells and are 90-70 times less cytotoxic than azidothymidine. The selectivity index of the compounds exceeds those of GA by 110 and 34 times, respectively.

机译：利用氨基酸的正丁酯或二肽的苄基酯合成了新的甘草酸（GA）共轭物。它们含有两个氨基酸残基（Met，Phe，Pro和Ile或二肽Gly-Leu和Gly-Phe）。 GA羧基的活化是在-羟基琥珀酰亚胺，-二环己基碳二亚胺或-羟基苯并三唑与二环己基碳二亚胺的帮助下进行的。含有脯氨酸的GA衍生物是一种低毒物质;与对照组相比，它使小鼠血液中凝集素水平提高了3.7倍，而溶血素水平提高了3倍。二肽GA衍生物在MT-4细胞培养物中具有抗HIV-1活性，其细胞毒性比叠氮胸苷低90-70倍。化合物的选择性指数分别比GA的选择性指数高110倍和34倍。

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期刊名称 Nature Public Health Emergency Collection
作者
L. A. Baltina; Jr.; R. M. Kondratenko; L. A. Baltina; N. Z. Baschenko; O. A. Pl’yasunova;
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作者单位

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年(卷),期 -1(35),4
年度 -1
页码 -1
总页数 8
原文格式 PDF
正文语种
中图分类精神病学;
关键词
glycyrrhizic acid; conjugates; amino acids; dipeptides; synthesis; immunostimulating and anti-HIV-1 activity;

机译：甘草酸;缀合物;氨基酸;二肽;合成;免疫刺激和抗HIV-1活性;

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专利

1. Synthesis and Biological Activity of New Glycyrrhizic Acid Conjugates with Amino Acids and Dipeptides [J] . Baltina LA, Kondratenko RM, Baltina LA, Russian journal of bioorganic chemistry . 2009,第4期

机译：新型甘草酸与氨基酸和二肽结合物的合成及生物活性
2. Synthesis and Antiviral Activity of Glycyrrhizic-Acid Conjugates with Aromatic Amino Acids [J] . A. I. Fairushina, L. A. Baltina, M. Yu. Eropkin, Chemistry of Natural Compounds . 2017,第6期

机译：甘草酸缀合物与芳族氨基酸的合成与抗病毒活性
3. Synthesis and Antiviral Activity of Novel Glycyrrhizic Acid Conjugates with D-Amino Acid Esters [J] . Fayrushina A. I., Baltina L. A. Jr., Baltina L. A., Russian journal of bioorganic chemistry . 2017,第4期

机译：二氨基酸酯的新型甘草酸缀合物的合成与抗病毒活性
4. 2-Oxoamides Based on Amino Acids and Dipeptides as Selective Phospholipase A_2 Inhibitors Presenting Anti-inflammatory Activity [C] . George Kokotos Chinese International Peptide Symposium . 2013

机译：基于氨基酸和二肽作为选择性磷脂酶A_2抑制剂呈现抗炎活性的2-氧氧酰胺
5. Part I. Application of 2-hydroxymethylacrylic acid, a product of Baylis-Hillman reaction, for the synthesis of novel N-backbone-to-side-chain cyclic peptide analogs: Strategies and side reactions. Part II. Synthesis and biological activities of chimeric bioactive peptides featuring amino acids coupled to 4-anilino-n-phenethyl-piperidine. [D] . Petrov, Ravil Rashitovich. 2007

机译：第一部分。Baylis-Hillman反应产物2-羟甲基丙烯酸在合成新型N骨架至侧链环状肽类似物中的应用：策略和副反应。第二部分具有与4-苯胺基-n-苯乙基-哌啶偶联的氨基酸的嵌合生物活性肽的合成和生物活性。
6. Synthesis and antiviral activity of novel glycyrrhizic acid conjugates with D-amino acid esters [O] . A. I. Fayrushina, L. A. Baltina, Jr., -1

机译：D-氨基酸酯类新型甘草酸缀合物的合成及抗病毒活性
7. Synthesis and biological activity of new glycyrrhizic acid conjugates with amino acids and dipeptides [O] . L. A. Baltina, R. M. Kondratenko, N. Z. Baschenko, 2009

机译：新甘草酸缀合物与氨基酸和二肽的合成与生物活性
8. Synthesis of Some N-Carboxy Methyl Amino Acid Esters and an Attempt to Prepare Di-(N-Carboxy Methyl Amino Acids Esters)-Sulphones for Possible Antimicrobial Activity [R] . Pasha, T. 1989

机译：一些N-羧甲基氨基酸酯的合成和尝试制备二 - （N-羧甲基氨基酸酯） - 可能的抗菌活性的手机

Synthesis and biological activity of new glycyrrhizic acid conjugates with amino acids and dipeptides

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