Synthesis and evaluation of enantiomeric quinoline-2-carboxamides: positron emission tomography imaging agents for the translocator protein.

ABSTRACT: The translocator protein (TSPO) is a key biomarker for inflammation. Positron emission tomography (PET) imaging of TSPO has emerged as a valuable tool for investigating multiple disorders throughout the body. We previously reported the development of [¹⁸F]LW223, a quinoline-2-carboxamide bearing an R-configured side chain, which binds TSPO independently of the rs6971 human polymorphism and enables quantification of macrophage-driven inflammation in the course of myocardial infarction. In the present study, we provide a comprehensive molecular and biological characterisation of LW223 and its S-enantiomer, further supporting their potential as PET imaging agents for human inflammatory processes. Two synthetic routes were developed: one enabling direct multigram-scale

SUBMITTER: Waddell LJN 

PROVIDER: S-EPMC12767876 | biostudies-literature | 2026 Feb

REPOSITORIES: biostudies-literature