Boron-containing compounds which possess unique and attractive properties have received increasing attention from the pharmaceutical industry and academia recently. They have shown interesting and useful biological activities, including antibacterial, antifungal, antiparasitic, antiviral, and anti-inflammatory activities. In this review, the synthetic strategies for various boron-containing compounds, including peptidyl boronic acids, benzoxaboroles, benzoxaborines, benzodiazaborines, amine carboxyboranes, and amine cyanoboranes are summarized. Representative structures of each structural class and recently developed biologically active boron-containing compounds are used as examples in this review.