[马来海松酸酰胺和臭氧分解产物的合成和药理活性]。

Bioorganicheskaia khimiia Pub Date : 2010-11-01
O B Kazakova, E V Tret'iakova, O S Kukovinets, G A Tolstikov, T I Nazyrov, I V Chudov, A F Ismagilova
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引用次数: 0

摘要

合成了一组含有氨基酸甲酯、脂肪胺、咪唑和n -甲基哌嗪片段的马来海松酸酰胺。马来酸甲酯的臭氧分解是通过双键C18(19)的断裂和无水循环的揭示而形成的二苯三酸。通过对马来海松酸衍生物抗炎、抗溃疡活性的筛选,发现了马来海松酸甲酯、臭氧分解产物二萜二三酸、马来海松酸酰胺等新的有效化合物。所研究的化合物的一个重要优点是低毒性和双向活性的存在,对动物没有不利影响。
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[Synthesis and pharmacological activity of amides and ozonolysis product of maleopimaric acid].

The synthesis of a new group of maleopimaric acid amides containing fragments of the methyl esters of amino acids, aliphatic amines, imidazole and N-methylpiperazine was carried out. Ozonolysis of methyl maleopimarate flows through the cleavage of double bond C18(19) and the disclosure of anhydrous cycle with formation of secotriacid. As a result of screening of anti-inflammatory and antiulcer activity of maleopimaric acid derivatives new effective compounds such as methyl esters of maleopimaric acid and product of ozonolysis - diterpenic secotriacid, maleopimaric acid amide with L-leucine were revealed. An important advantage of the compounds studied is the low toxicity and the presence of bidirectional activity in the absence of adverse effects on the animal.

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