利用2-乙氧基-1-乙氧羰基-1,2-二氢喹啉合成具有药理意义的甘草酸与氨基酸和二肽缀合物

IF 0.9 4区化学 Q4 CHEMISTRY, MEDICINAL

Chemistry of Natural Compounds Pub Date : 2025-09-19 DOI:10.1007/s10600-025-04791-3

A. I. Fairushina, S. F. Petrova, N. S. Makara, T. A. Sapozhnikova, L. A. Baltina

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引用次数: 0

摘要

提出了以2-乙氧基-1-乙氧羰基-1,2-二氢喹啉为原料，一步选择性制备甘草酸与氨基酸和二肽（L-Val、D-Val、L-Leu、D-Leu、L-Phe、D-Phe、Gly-Val、Gly-Leu、Gly-Phe）偶联物的方法，收率为60-65%。甘草酸与缬氨酸偶联物在50mg /kg剂量的吲哚美辛大鼠胃溃疡模型中表现出明显的抗溃疡活性。

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Synthesis of Pharmacologically Significant Conjugates of Glycyrrhizic Acid with Amino Acids and Dipeptides Using 2-Ethoxy-1-Ethoxycarbonyl-1,2-Dihydroquinoline

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Synthesis of Pharmacologically Significant Conjugates of Glycyrrhizic Acid with Amino Acids and Dipeptides Using 2-Ethoxy-1-Ethoxycarbonyl-1,2-Dihydroquinoline

A selective one-step method for preparing conjugates of glycyrrhizic acid (GA) with amino acids and dipeptides (L-Val, D-Val, L-Leu, D-Leu, L-Phe, D-Phe, Gly-Val, Gly-Leu, Gly-Phe) in 60–65% yields using 2-ethoxy-1-ethoxycarbonyl-1,2-dihydroquinoline was proposed. The conjugate of GA with valine exhibited pronounced antiulcer activity in a rat indomethacin gastric ulcer model at a dose of 50 mg/kg.

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来源期刊

Chemistry of Natural Compounds 化学-有机化学

CiteScore

1.40

自引率

25.00%

发文量

265

审稿时长

7.8 months

期刊介绍： Chemistry of Natural Compounds publishes reviews and general articles about the structure of different classes of natural compounds, the chemical characteristics of botanical families, genus, and species, to establish the comparative laws and connection between physiological activity and the structure of substances.