融合环丙烷在药物化学中的作用：来自过去十年的见解

IF 6 2区医学 Q1 CHEMISTRY, MEDICINAL

European Journal of Medicinal Chemistry Pub Date : 2025-07-08 DOI:10.1016/j.ejmech.2025.117951

Dongsheng Li

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引用次数: 0

摘要

由于融合环丙烷环具有固有的三维性、结构新颖性和独特的物理化学性质，在现代药物发现和药物化学活动中越来越普遍。本综述概述了过去十年来主要药物化学文献中的例子，以说明融合环丙烷环基序的不同应用，包括(a)增强代谢稳定性，(b)改善靶标结合能力，(c)新的化学型产生，(d)减少脱靶效应，(e)增加膜/血脑屏障（BBB）的通透性，(f)改善水解稳定性，(g)减轻毒性，(h)增强化学稳定性，(c)增强生物活性。(1)提高水溶性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

The roles of fused-cyclopropanes in medicinal chemistry: Insights from the past decade

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The roles of fused-cyclopropanes in medicinal chemistry: Insights from the past decade

Fused-cyclopropane rings have become increasingly prevalent in modern drug discovery and medicinal chemistry campaigns as they can provide inherent three-dimensionality, structural novelty, and unique physicochemical properties. This review presents an overview of examples from the primary medicinal chemistry literature over the past decade to illustrate diverse applications of fused-cyclopropane ring motifs, including (a) enhanced metabolic stability, (b) improved target binding potency, (c) novel chemotype generation, (d) reduced off-target effects, (e) increased membrane/blood-brain barrier (BBB) permeability, (f) improved hydrolytic stability, (g) mitigated toxicity liability, (h) enhanced chemical stability, and (i) improved aqueous solubility.

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来源期刊

European Journal of Medicinal Chemistry 化学-医药化学

CiteScore

11.70

自引率

9.00%

发文量

863

审稿时长

29 days

期刊介绍： The European Journal of Medicinal Chemistry is a global journal that publishes studies on all aspects of medicinal chemistry. It provides a medium for publication of original papers and also welcomes critical review papers. A typical paper would report on the organic synthesis, characterization and pharmacological evaluation of compounds. Other topics of interest are drug design, QSAR, molecular modeling, drug-receptor interactions, molecular aspects of drug metabolism, prodrug synthesis and drug targeting. The journal expects manuscripts to present the rational for a study, provide insight into the design of compounds or understanding of mechanism, or clarify the targets.