Preclinical Characterization of the Tau PET Tracer [F]SNFT-1: Comparison of Tau PET Tracers.

Tau PET tracers are expected to be sufficiently sensitive to track the progression of age-related tau pathology in the medial temporal cortex. The tau PET tracer -(4-[F]fluoro-5-methylpyridin-2-yl)-7-aminoimidazo[1,2-a]pyridine ([F]SNFT-1) has been successfully developed by optimizing imidazo[1,2-a]pyridine derivatives. We characterized the binding properties of [F]SNFT-1 using a head-to-head comparison with other reported F-labeled tau tracers.

Assessing the variability and correlation between SUV and ADC parameters of head and neck cancers derived from simultaneous PET/MRI: A single-center study.

Objective: Intratumoral heterogeneity is associated with poor outcomes in head and neck cancer (HNC) patients owing to chemoradiotherapy resistance. [ F]-FDG positron emission tomography (PET) / Magnetic Resonance Imaging (MRI) provides spatial information about tumor mass, allowing intratumor heterogeneity assessment through histogram analysis. However, variability in quantitative PET/MRI parameter measurements could influence their reliability in assessing patient prognosis.

Synthesis and evaluation of 2-pyrrolopyridinylquinoline derivatives as selective tau PET tracers for the diagnosis of Alzheimer's disease.

Introduction: [F]THK-5351 was originally developed as a positron emission tomography (PET) imaging tracer for the detection of accumulated tau proteins, the pathological hallmark of Alzheimer's disease (AD). However, clinical studies of [F]THK-5351 revealed the existence of off-target binding to monoamine oxidase-B (MAO-B). To overcome this off-target binding, in this work, we synthesized and evaluated 2-pyrrolopyridinylquinoline (PPQ) derivatives as selective tau PET imaging tracers.

F-SMBT-1: A Selective and Reversible PET Tracer for Monoamine Oxidase-B Imaging.

Reactive astrocytes play a key role in the pathogenesis of various neurodegenerative diseases. Monoamine oxidase-B (MAO-B) is one of the promising targets for the imaging of astrogliosis in the human brain. A novel selective and reversible MAO-B tracer, ()-(2-methylpyrid-5-yl)-6-[(3-F-fluoro-2-hydroxy)propoxy]quinoline (F-SMBT-1), was successfully developed via lead optimization from the first-generation tau PET tracer F-THK-5351.

Antimalarial activity of HIV-1 protease inhibitor in chromone series.

Increasing parasite resistance to nearly all available antimalarial drugs becomes a serious problem to human health and necessitates the need to continue the search for new effective drugs. Recent studies have shown that clinically utilized HIV-1 protease (HIV-1 PR) inhibitors can inhibit the in vitro and in vivo growth of Plasmodium falciparum. In this study, a series of chromone derivatives possessing HIV-1 PR inhibitory activity has been tested for antimalarial activity against P.