Biological Evaluation of d-[¹⁸F]Fluoroalanine and d-[¹⁸F]Fluoroalanine-d₃ as Positron Emission Tomography Imaging Tracers for Bacterial Infection.

ABSTRACT: d-Amino acids such as d-alanine are substrates for bacterial peptidoglycan biosynthesis and are selectively taken up by bacteria and not mammalian cells. Consequently, d-amino acid metabolism is an attractive target for antibiotic discovery and the development of bacteria-specific imaging agents. d-Fluoroalanine and the deuterium-labeled analogue fludalanine (MK641) were originally explored as antibiotics by Merck but failed in clinical trials due to unaccepted toxicity. Herein, we synthesized a fluorine-18 labeled d-fluoroalanine, d-3-[¹⁸F]fluoroalanine (d-[¹⁸F]FAla), and its deuterated analogue, d-3-[¹⁸F]fluoroalanine-d₃ (d-[¹⁸F]FAla-d₃), and evaluated their capability to image bacterial infection. Both d-[

SUBMITTER: Li K 

PROVIDER: S-EPMC11342404 | biostudies-literature | 2024 Aug

REPOSITORIES: biostudies-literature