Discovery of 1,3,4-oxadiazin-5-one Derivative CJ1-34 as a Partial ATP Synthase Inhibitor for CNS Applications.

ATP synthase dysregulation has been implicated in many diseases, including cancer and neurodegenerative diseases. Whilst ATP synthase-targeting compounds have been reported, most are large or polar compounds and lack appropriate properties for a CNS drug. We designed, synthesised, and evaluated a novel series of ATP synthase targeting compounds, resulting in a 1,3,4-oxadiazin-5-one scaffold with improved physiochemical properties.

Coblation as an effective tool for treating subglottic cysts and hemangiomas in pediatric patients.

Subglottic cysts and hemangiomas are rare but potentially life-threatening conditions in pediatric patients. Subglottic cysts are generally associated with premature infants with a history of prolonged endotracheal intubation, while subglottic hemangiomas are congenital vascular lesions that grow rapidly and are uncommon head and neck tumours in pediatric patients. Both conditions can present with generalised respiratory symptoms such as stridor.

Vitamin D status and its determinants in German elite athletes.

Purpose: This study investigated elite German athletes to (1) assess their serum 25(OH)D levels and the prevalence of insufficiency, (2) identify key factors influencing serum 25(OH)D levels, and (3) analyze the association between serum 25(OH)D levels and handgrip strength.

Methods: In this cross-sectional study, a total of 474 athletes (231 female), aged 13-39 years (mean 19.3 years), from ten Olympic disciplines were included.

Exploration of (R)-[C]YH168 as a PET tracer for imaging monoacylglycerol lipase in the brain: from mice to non-human primates.

Purpose: The monoacylglycerol lipase (MAGL) plays a pivotal role in modulating the endocannabinoid system and is considered an attractive therapeutic target for diseases in both the central nervous system and periphery. The current study aimed to develop and evaluate a suitable carbon-11 labeled tracer for imaging MAGL in preclinical studies.

Methods: (R)-YH168 was synthesized via a multi-step pathway and its half-maximal inhibitory concentration (IC) values were measured using an enzymatic assay.

Antiviral drug discovery with an optimized biochemical dengue protease assay: Improved predictive power for antiviral efficacy.

The viral NS2B-NS3 protease is a promising drug target to combat dengue virus (DENV) and other emerging flaviviruses. The discovery of novel DENV protease inhibitors with antiviral efficacy is hampered by the low predictive power of biochemical assays. We herein present a comparative evaluation of biochemical DENV protease assay conditions and their benchmarking against antiviral efficacy and a protease-specific reporter gene assay.