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新型吡咯生物碱类似物的设计、合成与抗真菌活性。

Design, synthesis and antifungal activities of novel pyrrole alkaloid analogs.

机构信息

State Key Laboratory of Elemento-Organic Chemistry, Research Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, China.

出版信息

Eur J Med Chem. 2011 May;46(5):1463-72. doi: 10.1016/j.ejmech.2011.01.031. Epub 2011 Jan 28.

DOI:10.1016/j.ejmech.2011.01.031
PMID:21356570
Abstract

A series of novel analogs of pyrrole alkaloid were designed and synthesized by a facile method and their structures were characterized by 1H NMR, 13C NMR and high-resolution mass spectrometry (HRMS). The structure of compound 2a was identified by 2D NMR including heteronuclear multiple-quantum coherence (HMQC), heteronuclear multiple-bond correlation (HMBC) and H-H correlation spectrometry (H-H COSY) spectra. Their antifungal activities against five fungi were evaluated, and the results indicated that some of the title compounds showed moderate fungicidal activities in vitro against Alternaria solani, Cercospora arachidicola, Fusarium omysporum, Gibberella zeae and Physalospora piricola at the dosage of 50 μg mL(-1). Compound 2a and 3a exhibited good activities against P. piricola at low dosage.

摘要

通过一种简便的方法设计并合成了一系列新型吡咯生物碱类似物,通过 1H NMR、13C NMR 和高分辨率质谱(HRMS)对其结构进行了表征。通过包括异核多量子相干(HMQC)、异核多键相关(HMBC)和 H-H 相关光谱(H-H COSY)在内的二维 NMR(2D NMR)确定了化合物 2a 的结构。评估了它们对五种真菌的抗真菌活性,结果表明,一些标题化合物在 50 μg mL(-1)的剂量下对茄腐镰孢菌、花生褐斑病菌、尖孢镰刀菌、玉蜀黍赤霉菌和梨叶点霉具有中等体外杀菌活性。化合物 2a 和 3a 在低剂量下对梨叶点霉表现出良好的活性。

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