The term privileged structure was first coined by Evans et al. in 1988 and was defined as “a single molecular framework able to provide ligands for diverse receptors”. This group noted the ability of 1,4benzodiazepin-2-ones to bind to cholecystokinin (CCK) (such as 1), gastrin, and central benzodiazepine receptors (such as 2) (Figure 1).1 In addition to these, the benzodiazepine scaffold is also found as neurokinin-1 antagonists (3), as enzyme inhibitors such as κ-secretase inhibitors (4) and farnesyl:protein transferase inhibitors (5), and as ion channel ligands such as the delayed rectifier K+ current modulator 6.3,4