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抗生素利福霉素衍生物利法米昔的多态性-结构关系

Polymorphism-structure relationships of rifamexil, an antibiotic rifamycin derivative.

作者信息

Bacchi A, Mori G, Pelizzi G, Pelosi G, Nebuloni M, Panzone G B

机构信息

Dipartimento di Chimica Generale ed Inorganica, Chimica Analitica, Chimica Fisica, Parma, Italy.

出版信息

Mol Pharmacol. 1995 Mar;47(3):611-23.

PMID:7700258
Abstract

The polymorphism of rifamexil, a rifamycin derivative, has been investigated by thermomicroscopy, differential thermal analysis (differential scanning calorimetry-thermogravimetry), IR spectroscopy, and X-ray powder diffraction. Two crystalline forms, an amorphous material, and three solvates have been studied. The crystal structures of two solvates have also been determined by single-crystal X-ray techniques. Although the overall conformation of rifamexil is very similar in the two compounds, marked differences occur between the two crystal packings, due to differences both in the mutual orientation of the molecules and in the rifamexil-solvent interactions. Multivariate statistical methods have been used to identify the principal structural parameters determining the biological activity of the rifamycins.

摘要

利福米昔(一种利福霉素衍生物)的多晶型现象已通过热显微镜、差示热分析(差示扫描量热法 - 热重分析法)、红外光谱和X射线粉末衍射进行了研究。已对两种晶型、一种无定形物质和三种溶剂化物进行了研究。两种溶剂化物的晶体结构也已通过单晶X射线技术确定。尽管利福米昔在这两种化合物中的整体构象非常相似,但由于分子的相互取向以及利福米昔与溶剂相互作用的差异,两种晶体堆积之间存在明显差异。已使用多变量统计方法来确定决定利福霉素生物活性的主要结构参数。

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