Alzheimer’s disease (AD) is a chronic neurodegenerative disorder and the most common
cause of dementia among the elderly population. The good correlation of the density and …

Advanced leads from a series of 1,2,4-triazolo[4,3-a]pyridines with mGlu2 receptor PAM
activity are reported. By modification of the analogous imidazo[1,2-a]pyridine series, the newly …

The P2X7 receptor (P2X7R) orchestrates neuroinflammation, and this is the basis for an
increased interest in the development of antagonists inhibiting P2X7R function in the brain. This …

In this study, we have synthesized and evaluated 18 F-JNJ64349311, a tracer with high affinity
for aggregated tau (inhibition constant value, 8 nM) and high (≥500×) in vitro selectivity …

The synthesis and in vitro and in vivo evaluation of a new series of 7-(phenylpiperidinyl)-1,2,4-triazolo[4,3-a]pyridines,
which were conveniently radiolabeled with carbon-11, as …

Advanced leads of an imidazopyridine series of positive allosteric modulators of the metabotropic
glutamate 2 (mGlu2) receptor are reported. The optimization of in vitro ADMET and in …

We previously reported the discovery of 4-aryl-substituted pyridones with mGlu2 PAM activity
starting from the HTS hit 5. In this article, we describe a different exploration from 5 that led …

A novel series of pyrido[4,3-e][1,2,4]triazolo[4,3-a]pyrazines is reported as potent PDE2/PDE10
inhibitors with drug-like properties. Selectivity for PDE2 was obtained by introducing a …

Phosphodiesterases are enzymes that inactivate the intracellular second messengers 3′,5′-cyclic
adenosine-monophosphate and/or cyclic guanosine-monophosphate. Of all 11 …

A mini-HTS on 4000 compounds selected using 2D fragment-based similarity and 3D
pharmacophoric and shape similarity to known selective tau aggregate binders identified N-(6-…