Design, synthesis and structure-activity relationships of novel benzoxazolone derivatives as 18Â kDa translocator protein (TSPO) ligands

Benzoxazolone derivatives were designed and synthesized as novel TSPO ligands. In view of initial SAR study, we selected compound 14 as lead compound. Further optimization of pharmacokinetic properties of compounds led to discovery of compound 74 which exhibited anxiolytic effect in the rat Vogel model.