Conotoxins, the disulfide-rich toxin components of venomous marine cone snails, have attracted a great deal of attention in recent years because of their demonstrated pharmacological receptor subtype selectivities and distinct potential for development as new central nervous system (CNS) therapeutics. This review highlights some of the recent advancements in this field and describes a selection of contemporary papers pertaining to regioselective strategies for the synthesis of disulfide bridges in conotoxins, as well as other small constrained peptides. Primarily, we have covered papers that have appeared in the scientific literature over the past two years. A number of comprehensive conotoxin literature reviews have appeared in recent times.