Macrocyclization strategy for improving candidate profiles in medicinal chemistry,European Journal of Medicinal Chemistry

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Macrocyclization strategy for improving candidate profiles in medicinal chemistry
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2024-05-14 , DOI: 10.1016/j.ejmech.2024.116501
Om Darlami ₁ , Rabin Pun ₁ , Sung-Hoon Ahn ₂ , Seok-Ho Kim ₂ , Dongyun Shin ₁

Affiliation

Macrocycles are defined as cyclic compounds with 12 or more members. In medicinal chemistry, they are categorized based on their core chemistry into cyclic peptides and macrocycles. Macrocycles are advantageous because of their structural diversity and ability to achieve high affinity and selectivity towards challenging targets that are often not addressable by conventional small molecules. The potential of macrocyclization to optimize drug-like properties while maintaining adequate bioavailability and permeability has been emphasized as a key innovation in medicinal chemistry. This review provides a detailed case study of the application of macrocyclization over the past 5 years, starting from the initial analysis of acyclic active compounds to optimization of the resulting macrocycles for improved efficacy and drug-like properties. Additionally, it illustrates the strategic value of macrocyclization in contemporary drug discovery efforts.

中文翻译：

改善药物化学候选谱的大环化策略

大环被定义为具有12个或更多成员的环状化合物。在药物化学中，它们根据其核心化学性质分为环肽和大环化合物。大环化合物具有优势，因为它们的结构多样性以及对传统小分子通常无法解决的具有挑战性的目标实现高亲和力和选择性的能力。大环化在优化药物特性的同时保持足够的生物利用度和渗透性的潜力已被强调为药物化学的关键创新。本综述提供了过去 5 年大环化应用的详细案例研究，从无环活性化合物的初步分析到优化所得大环化合物以提高功效和类药特性。此外，它还说明了大环化在当代药物发现工作中的战略价值。

更新日期：2024-05-14

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