25 research outputs found

    Identification of a Novel Benzoxazolone Derivative as a Selective, Orally Active 18 kDa Translocator Protein (TSPO) Ligand

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    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
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