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Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
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Unlike ionic or small covalent molecules, polymers do not form crystalline solids due to the diffusion limitations of their long-chain structures. However, polymers contain microscopic crystalline domains separated by amorphous domains.
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хлорфенапир晶体多态性和杀虫活性

Reese Aronin1, Petr Brázda2, Leilani N Smith1

  • 1Department of Chemistry and Molecular Design Institute, New York University, 29 Washington Place, New York City, New York 10003, United States.

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概括

鉴定出了杀虫剂二的四种晶体形式. 虽然多态体对果和蚊子具有相似的致命性,但生物可用性各不相同,使杀虫活性预测复杂化.

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科学领域:

  • 农业科学 农业科学
  • 材料科学 材料科学 材料科学
  • 杀虫剂开发 杀虫剂开发

背景情况:

  • хлорфенапир 是一种需要代谢激活的益虫杀虫剂.
  • 了解其晶体形式 (多态) 对于优化疗效至关重要.
  • 多态性可以影响物理性质和生物可用性.

研究的目的:

  • 为了识别和表征fenapyr 的结晶多态.
  • 为了评估不同二多态的杀虫活性.
  • 为了研究二烯结构,生物可用性和杀虫活性之间的关系.

主要方法:

  • 极化的光光学显微镜.
  • 不同扫描热量计差异扫描热量计.
  • 拉曼光谱法 拉曼光谱法
  • 在X射线中,X射线的衍射效果是不同的.
  • 电子衍射的电子衍射方式
  • 对Drosophila melanogaster和Anopheles quadrimaculatus进行致死性测定

主要成果:

  • 鉴定出了四种二的结晶多态,其中三种是多类型的.
  • 所有多形体对果和蚊子都表现出类似的致命性.
  • 最不稳定的多态体表现出略高的致命性.
  • 淘汰动力学受到内部代谢激活步骤的影响,影响生物可用性.

结论:

  • хлорфенапир表现出多态性,具有明显的晶体结构.
  • 虽然结构相似性表明可比的杀虫活性,但生物可用性差异使直接相关性复杂化.
  • 需要进一步的研究来阐明代谢激活对多形态依赖生物可用性和疗效的影响.