Lecture «Annelated medium-sized nitrogen heterocycles as suitable scaffolds for cns-targeted leads»

Medium-sized nitrogen heterocycles (7-to-15-membered) have widespread interest in organic synthesis and medicinal chemistry. These heterocyclic rings are found as subunits or core structures in natural and bioactive molecules, including pharmaceutical products, whereas on the other hand they often serve as key intermediates in the synthesis of bicyclic compounds by selective transformations (e.g., transannular ring-contractions, cycloadditions). These molecular frameworks, particularly annelated 7-to-10-membered aza-heterocycles, have drawn attention as potential scaffolds for developing new multitarget-directed ligands (MTDLs) for treating Alzheimer’s disease (AD) and other related neurodegenerative syndromes.

Starting from our findings on the suitability of partially hydrogenated annelated azepine and azocine derivatives targeted at enzymes, receptors and biochemical pathways involved in the pathogenesis of AD, we extended the investigation to novel derivatives of annelated 7-to-10-membered nitrogen heterocycles targeted AD-associated targets (e.g., butyryl- and acetylcholinesterase, monoamine oxidases A and B, Aβ aggregation, ROS insult, NMDAR antagonism). The results from the investigation on cell and ex vivo/in vivo animal models will be discussed in an effort of progressing drug optimization of CNS-targeted aza-heterocyclic lead compounds.

The event will start at 15:00