V2EX bioisostere

Bioisostere

定义 Definition

bioisostere(生物等排体 / 生物等排基):在药物化学中,指在大小、形状、电子性质等方面相似、并且在生物体系中能产生相近药理作用或结合行为的原子、基团或分子片段。常用于“等排替换(bioisosteric replacement)”以优化药物的效力、选择性、代谢稳定性、溶解度或安全性。(该词在不同语境下也可有更广义/更狭义的用法。)

发音 Pronunciation

/ba.oa.s.str/

例句 Examples

A fluorine atom is sometimes used as a bioisostere for hydrogen in drug design.
在药物设计中,氟原子有时会被用作氢的生物等排体。

By replacing an amide with a bioisostere, the team improved metabolic stability while keeping similar binding to the target enzyme.
通过用生物等排体替换酰胺基团,团队在保持对靶酶相近结合能力的同时,提高了代谢稳定性。

词源 Etymology

该词由 bio-(生物的) + isostere(等排体) 组成。Isostere 源自希腊语词根 iso-(相同)stereos(立体的、坚实的;引申为“空间/立体特征”)/strong>,最初用于描述在物理化学性质上相近、可相互替换的原子或基团;加入 bio- 后强调这种“可替换性”是在生物活性与药效表现层面成立,常见于现代药物化学与先导化合物优化。

相关词 Related Words

文学/著作中的用例 Literary Works

  • Foye’s Principles of Medicinal Chemistry(药物化学经典教材,常在结构优化与等排替换章节讨论 bioisostere)
  • The Practice of Medicinal Chemistry(系统介绍药物研发实践,包含 bioisosteric replacement 的策略与案例)
  • An Introduction to Medicinal Chemistry(入门级药物化学教材,常用 bioisostere 解释活性与性质优化)
  • Burger’s Medicinal Chemistry and Drug Discovery(大型参考书,涉及生物等排体在先导优化中的应用)
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