Harry John Wadsworth

TL;DR: The design and synthesis of novel azabicyclic methyl esters as ligands for the muscarinic receptor are described, which generally show improved affinity relative to the corresponding methyl ester.

TL;DR: There is a close correlation between the activity of the benzofurans as inhibitors of fibril formation and their ability to bind to beta-amyloid, as identified by scintillation proximity binding assay and NMR studies.

TL;DR: A series of tricyclic compounds have been synthesised and evaluated in vitro for affinity against Translocator protein 18 kDa (TSPO) and for preferred imaging properties and the most promising of the compounds were radiolabelled and evaluated for biodistribution and specificity for high expressing TSPO regions.

TL;DR: A relationship between position and depth of the electrostatic minima relative to the azabicyclic ring and the potency and efficacy of the compounds was determined.

TL;DR: These compounds provide muscarinic ligands with high potency and a range of efficacies suitable for testing as candidate drugs in the treatment of Alzheimer's disease.