Fluorine-Containing Macrocyclic Peptides and Peptidomimetics

IF 4.6 1区化学 Q1 CHEMISTRY, ORGANIC

Organic Chemistry Frontiers Pub Date : 2025-05-06 DOI:10.1039/d5qo00219b

Stefan Roesner, Neshat Rozatian

引用次数: 0

Abstract

Fluorination plays a vital role in medicinal chemistry due to the unique properties of the fluorine atom. Macrocyclic peptides offer advantageous properties compared to linear peptides in drug discovery. In recent years, the development of fluorinated macrocyclic peptides and peptidomimetics, such as voxilaprevir, MK-0616 and ulimorelin, has highlighted the growing interest in the combination of fluorination and cyclization for tuning the properties of peptidic drug leads. In this review, the effects of fluorination upon biological properties of macrocyclic peptides will be discussed. The use of the fluorine atom as a ¹⁹F NMR spectroscopy probe for conformational studies of macrocyclic peptides will be reviewed. Finally, macrocyclic peptides containing the radionucleotide ¹⁸F as PET imaging agents will be highlighted.

查看原文本刊更多论文

含氟大环肽和拟肽物

由于氟原子的独特性质，氟化在药物化学中起着至关重要的作用。与线性肽相比，大环肽在药物发现方面具有优势。近年来，氟化大环肽和类肽制剂的发展，如伏西拉韦、MK-0616和乌莫瑞林，突显了人们对氟化和环化结合以调整肽类药物先导物性质的兴趣日益浓厚。本文就氟化对大环肽生物学特性的影响作一综述。本文将对氟原子作为19F核磁共振光谱探针在大环肽构象研究中的应用进行综述。最后，将重点介绍含有放射性核苷酸18F的大环肽作为PET显像剂。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

求助全文

约1分钟内获得全文求助全文

来源期刊

Organic Chemistry Frontiers CHEMISTRY, ORGANIC-

CiteScore

7.90

自引率

11.10%

发文量

686

审稿时长

1 months

期刊介绍： Organic Chemistry Frontiers is an esteemed journal that publishes high-quality research across the field of organic chemistry. It places a significant emphasis on studies that contribute substantially to the field by introducing new or significantly improved protocols and methodologies. The journal covers a wide array of topics which include, but are not limited to, organic synthesis, the development of synthetic methodologies, catalysis, natural products, functional organic materials, supramolecular and macromolecular chemistry, as well as physical and computational organic chemistry.