Automated synthesis of oligosaccharides as a basis for drug discovery

Carbohydrates present both potential and problems — their biological relevance has been recognized, but problems in procuring sugars rendered them a difficult class of compounds to handle in drug discovery efforts. The development of the first automated solid-phase oligosaccharide synthesizer and other methods to assemble defined oligosaccharides rapidly has fundamentally altered this situation. This review describes how quick access to oligosaccharides has not only contributed to biological, biochemical and biophysical investigations, but also to drug discovery. Particular focus will be placed on the development of carbohydrate-based vaccines, defined heparin oligosaccharides and aminoglycosides that have recently begun to affect drug discovery.