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锥虫杀灭剂埃瑞曼托内酯C氧化物衍生物的¹H和¹³C核磁共振数据的完整归属

Complete assignments of 1H and 13C NMR data for trypanocidal eremantholide C oxide derivatives.

作者信息

Saúde-Guimarães Dênia A, Perry Katia S P, Raslan Délio S, Chiari Egler, Barrero Alejandro F, Oltra Juan E

机构信息

LAPLAMED, DEFAR, Escola de Farmácia, Universidade Federal de Ouro Preto, Rua Costa Sena, 171, CEP 35400-000, Ouro Preto, Minas Gerais, Brazil.

出版信息

Magn Reson Chem. 2007 Dec;45(12):1084-7. doi: 10.1002/mrc.2093.

DOI:10.1002/mrc.2093
PMID:18044809
Abstract

The chemical transformations of eremantholide C (1), a trypanocidal sesquiterpene lactone isolated from Lychnophora trichocarpha Spreng., gave five new oxide derivatives: 3'-hydroxyeremantholide C (2), 1'-formyleremantholide C (3), 1'-carboxyeremantholide C (4), 1'-carbomethoxyeremantholide C (5) and sodium 1'-carboxylate of eremantholide C (6). The (1)H and (13)C NMR data of all these derivatives were assigned based on 1D and 2D techniques. The derivatives were evaluated against Y and CL strains of Trypanosoma cruzi. All of them were inactive against the Y strain. Compounds 2 and 5 displayed 100% activity on the CL strain while compounds 4 and 6 were partially active on the CL strain.

摘要

从毛果灯台莲(Lychnophora trichocarpha Spreng.)中分离得到的具有杀锥虫活性的倍半萜内酯埃瑞曼索内酯C(1)发生化学转化,得到了5种新的氧化物衍生物:3'-羟基埃瑞曼索内酯C(2)、1'-甲酰基埃瑞曼索内酯C(3)、1'-羧基埃瑞曼索内酯C(4)、1'-甲氧基羰基埃瑞曼索内酯C(5)和埃瑞曼索内酯C的1'-羧酸钠(6)。所有这些衍生物的氢谱(1H)和碳谱(13C)数据均基于一维(1D)和二维(2D)技术进行了归属。对这些衍生物针对克氏锥虫的Y株和CL株进行了评估。它们对Y株均无活性。化合物2和5对CL株显示出100%的活性,而化合物4和6对CL株具有部分活性。

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