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抗恰加斯病剂 (E)-苯乙烯基苯并呋咱固体状态的结构关系。

Structural relationships in the solid state of the anti-chagas agent (E)-phenylethenylbenzofuroxan.

机构信息

Instituto de Física de São Carlos, Universidade de São Paulo, CP 369, Sao Carlos, 13560-970, SP, Brazil.

出版信息

Mol Divers. 2010 Nov;14(4):643-52. doi: 10.1007/s11030-009-9202-4. Epub 2009 Nov 10.

DOI:10.1007/s11030-009-9202-4
PMID:19902372
Abstract

The crystal structure and the vibrational spectrum of a potential drug for Chagas's disease treatment, the (E)-isomer of phenylethenylbenzofuroxan 1 (5(6)(E)-[(2-phenylethenyl)]benzo[1,2-c]1,2,5-oxadiazole N-oxide), are reported. In order to provide insights into structural relationships, quantum mechanical calculations were employed starting from crystal structure. These results have given theoretical support to state interesting structural features, such as the effect of some intermolecular contacts on the molecule conformation and the electronic delocalization decreasing through atoms of the benzofuroxan moiety. Furthermore, the MOGUL comparative analysis in the Cambridge Structural Database provided additional evidences on these structural behaviors of compound 1. Intermolecular contacts interfere on the intramolecular geometry, as, for instance, on the phenyl group orientation, which is twisted by 12.32(6)° from the ethenylbenzofuroxan plane. The experimental Raman spectrum of compound 1 presents unexpected frequency shift and also anomalous Raman activities. At last, the molecule skeleton deformation and the characteristic vibrational modes were correlated by matching the experimental Raman spectrum to the calculated one.

摘要

报道了一种用于恰加斯病治疗的潜在药物的(E)-对苯基乙烯基苯并呋咱异构体 1(5(6)(E)-[(2-对苯基乙烯基)]苯并[1,2-c]1,2,5-恶二唑 N-氧化物)的晶体结构和振动光谱。为了深入了解结构关系,我们从晶体结构出发,采用量子力学计算进行了研究。这些结果为一些有趣的结构特征提供了理论支持,例如一些分子间相互作用对分子构象的影响以及苯并呋咱部分原子的电子离域程度降低。此外,MOGUL 在剑桥结构数据库中的比较分析为化合物 1 的这些结构行为提供了更多证据。分子间相互作用会干扰分子内的几何形状,例如,对乙烯基苯并呋咱平面的扭曲,扭曲角度为 12.32(6)°。化合物 1 的实验拉曼光谱呈现出意想不到的频率位移和异常拉曼活性。最后,通过将实验拉曼光谱与计算结果进行匹配,将分子骨架变形与特征振动模式相关联。

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