A sizeable proportion of currently marketed drugs come from heterocycles. The heterocyclic moiety 5-pyrazolone is well known five-membered ring containing nitrogen. Derivatives of this wonder nucleus have exhibited activities as diverse as antimicrobial, anti-inflammatory, analgesic, antidepressant, anticonvulsant, antidiabetic, antihyperlipidemic, antiviral, antitubercular, antioxidant, anticancer and antiviral, including action against severe acute respiratory syndrome (SARS) or 3C protease inhibitor. A number of drugs based on this motif have already made it to the market. Standard texts and literature on medicinal chemistry cite different approaches for the synthesis of 5- pyrazolones. The present review provides an insight view to 5-pyrazolone synthesis, their biological profile and structure-activity relationship studies.

目前上市的药物中有很大一部分来自杂环。杂环部分5-吡唑啉酮是众所周知的含氮五元环。这个神奇核的衍生物表现出多种活性，如抗菌、抗炎、镇痛、抗抑郁、抗惊厥、抗糖尿病、抗高血脂、抗病毒、抗结核、抗氧化、抗癌和抗病毒，包括对严重急性呼吸系统综合症 (SARS) 或 3C 蛋白酶的作用抑制剂。许多基于该主题的药物已经上市。关于药物化学的标准教科书和文献引用了合成 5-吡唑啉酮的不同方法。本综述提供了对 5-吡唑啉酮合成、其生物学特征和构效关系研究的深入了解。