Fluorine-containing macrocyclic peptides and peptidomimetics

Rozatian, N and Roesner, S ORCID: 0000-0003-2143-4708 (2025) Fluorine-containing macrocyclic peptides and peptidomimetics. Organic Chemistry Frontiers, 12 (17). pp. 4871-4895. ISSN 2052-4110

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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 on 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.

Item Type:	Article
Uncontrolled Keywords:	3405 Organic Chemistry; 34 Chemical Sciences; Biotechnology; Biomedical Imaging; 0305 Organic Chemistry; 3405 Organic chemistry; 3405 Organic Chemistry; 34 Chemical Sciences; Biotechnology; Biomedical Imaging; 0305 Organic Chemistry; 3405 Organic chemistry
Subjects:	Q Science > QD Chemistry R Medicine > RS Pharmacy and materia medica
Divisions:	Pharmacy and Biomolecular Sciences
Publisher:	Royal Society of Chemistry
Date of acceptance:	2 May 2025
Date of first compliant Open Access:	10 September 2026
Date Deposited:	10 Sep 2026 14:47
Last Modified:	10 Sep 2026 14:47
DOI or ID number:	10.1039/d5qo00219b
URI:	https://researchonline.ljmu.ac.uk/id/eprint/29387

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