Department of Chemistry, Faculty of Basic and Applied Science, Madhav University, Sirohi, Rajasthan, India.
Piramal Pharma Limited-Discovery Solutions, Ahmedabad, Gujarat, India.
Arch Pharm (Weinheim). 2021 Nov;354(11):e2100062. doi: 10.1002/ardp.202100062. Epub 2021 Jun 29.
Azetidines are almost unexplored among nitrogen-containing saturated heterocycles due to difficulties associated with their synthesis. However, over the past few years, attempts have been made by scientists to advance their synthetic feasibility. Compounds with the azetidine moiety display an important and diverse range of pharmacological activities, such as anticancer, antibacterial, antimicrobial, antischizophrenic, antimalarial, antiobesity, anti-inflammatory, antidiabetic, antiviral, antioxidant, analgesic, and dopamine antagonist activities, and are also useful for the treatment of central nervous system disorders and so forth. Owing to its satisfactory stability, molecular rigidity, and chemical and biological properties, azetidine has emerged as a valuable scaffold and it has drawn the attention of medicinal researchers. The present review sheds light on the traditional method of synthesis of azetidine and advancements in synthetic methodology over the past few years, along with its application with various examples, and its biological significance.
氮杂环丁烷由于其合成困难，在含氮饱和杂环中几乎未被探索。然而，在过去的几年中，科学家们已经尝试提高其合成的可行性。具有氮杂环丁烷部分的化合物表现出重要且多样的药理学活性，如抗癌、抗菌、抗微生物、抗精神分裂症、抗疟疾、抗肥胖、抗炎、抗糖尿病、抗病毒、抗氧化、镇痛和多巴胺拮抗剂活性，并且还可用于治疗中枢神经系统疾病等。由于其令人满意的稳定性、分子刚性以及化学和生物学性质，氮杂环丁烷已成为一种有价值的支架，并引起了药物研究人员的关注。本综述介绍了氮杂环丁烷的传统合成方法以及过去几年中合成方法的进展，以及其在各种实例中的应用及其生物学意义。
