Sigma (σ) receptors are involved in several functions such as modulation and biosynthesis of several neurotransmitters, motor control, cell growth and proliferation [1]. The lack of any endogenous ligand and the existence of at least two sigma receptors subtypes σ1 and σ2 make it difficult to characterize their biological role. The interest for σ ligands stems from the possibility to develop clinical agents for the treatment of several CNS diseases (affective and motor disorders, cocaine abuse, cognitive impairment), for neuroprotection, tumor treatment and diagnosis[2]. The σ2 receptor agonists results in morphological changes and apoptosis in various cell lines, including breast tumor cells. Thus, σ2 receptors may be involved in regulating cell growth and proliferation.
Several classes of structurally unrelated compounds interact with σ receptors, but only few σ2 ligands are known.
With the aim to obtain new σ selective ligands, we synthesized some benzooxazol-2-one and benzooxazol-2-thione (1 and 2) derivatives.
