Antibiotics have served the mankind more than any other class of therapeutics. Since the first known use of antibiotics more than 2500 years ago, intensive research studies in the field led to development of numerous broad-spectrum antibacterial agents. The clinical application of these molecules led to decrease in mortality rate significantly. This resulted into diminished interest in research on antibiotics by the end of 20th century. However, the development of resistant strains of bacteria worldwide led to revival of research interest in the field. The development of knowledge on synthetic and metabolic pathways and resistance mechanism has led to discovery of several new antibacterial agents. This chapter discusses the challenges and opportunities in development of four important classes of carbohydrate-containing antibiotics – aminoglycosides, nucleosides, macrolides and glycopeptides. It gives an outline of the recently published novel isolated, semi-synthetic as well as synthetic molecules, their mechanism of action, if known, and the strategies for the design of compounds with potential antibacterial properties.

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