Macrocycles cover a small segment of molecules with a vast range of biological activity in the chemotherapeutic world. Primarily, the natural sources derived from macrocyclic drug candidates with a wide range of biological activities are known. Further evolutions of the medicinal chemistry towards macrocycle-based chemotherapeutics involve the functionalization of the natural product by hemisynthesis. More recently, macrocycles based on carbohydrates have evolved a considerable interest among the medicinal chemists worldwide. Carbohydrates provide an ideal scaffold to generate chiral macrocycles with well-defined pharmacophores in a decorated fashion to achieve the desired biological activity. We have given an overview on carbohydrate-derived macrocycle involving their synthesis in drug design and discovery and potential role in medicinal chemistry.

大环化合物在化学治疗领域覆盖了一小部分具有广泛生物活性的分子。首先，已知具有大范围生物活性的来源于大环候选药物的天然来源。药物化学向基于大环化合物的化学疗法的进一步发展涉及通过半合成对天然产物进行功能化。最近，基于碳水化合物的大环化合物在全世界的药物化学家中引起了相当大的兴趣。碳水化合物提供了一种理想的支架，可以以修饰的方式生成带有定义明确的药效基团的手性大环化合物，以实现所需的生物活性。