25 research outputs found
Identification of a Novel Benzoxazolone Derivative as a Selective, Orally Active 18 kDa Translocator Protein (TSPO) Ligand
Optimization
of the pharmacokinetic properties for a series of
benzoxazolone derivatives led to the identification of <b>9b</b>, which showed anxiolytic effect in a rat model. However, <b>9b</b>, like known benzodiazepines, induced motor impairment. Investigation
into the cause of this unexpected side effect and management of <b>9b</b> off-target binding affinity led to the identification of <b>10d</b>, which showed oral anxiolytic effect in the rat model
with improved safety profile