Lab of Chemical Biology and Molecular Drug Design, College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou, 310014, China.
Lab of Molecular Immunology, Virus Inspection Department, Zhejiang Provincial Center for Disease Control and Prevention, Hangzhou, 310051, China.
Mini Rev Med Chem. 2018;18(11):948-961. doi: 10.2174/1389557516666160928162724.
At present, diseases resulting from various reasons have been causing deadly fears to humans and previously incogitable losses to health. Meanwhile, the patient compliance has been weakening because of drug resistance and serious drug adverse effects. There is therefore an urgent need for the development of novel structural agents. Rhodanine derivatives have exhibited wide biological activities, as well as significant industrial applications, which suggests that rhodanine heterocycle represents a key structural motif in heterocyclic chemistry and occupies a prominent position in drug discovery. Here, we review some deadly defects of clinical medicines to the therapy of diseases and important advances on rhodanine derivatives in drug researches (e.g. as anti-diabetic, anti-viral, antiinflammatory, anti-microbial, anti-tumor agents and inhibitors for Alzheimer Disease), indicating that rhodanine heterocycle could be used as a significant pharmacophore to develop novel pharmacological active molecules. It is believed that the review is of importance for new ideas in the development of and rational designs of rhodanine-based drugs.
目前,由于各种原因导致的疾病一直给人类带来致命的恐惧和前所未有的健康损失。同时,由于耐药性和严重的药物不良反应,患者的依从性正在减弱。因此,迫切需要开发新型结构药物。由于拥有广泛的生物活性以及重要的工业应用价值,硫代吗啉衍生物在药物研究中备受关注(如作为抗糖尿病、抗病毒、抗炎、抗菌、抗肿瘤药物和阿尔茨海默病抑制剂),这表明硫代吗啉杂环代表了杂环化学中的一个关键结构基序,并在药物发现中占据着重要地位。在这里,我们回顾了一些临床药物在治疗疾病方面的致命缺陷,以及硫代吗啉衍生物在药物研究方面的重要进展(如抗糖尿病、抗病毒、抗炎、抗菌、抗肿瘤药物和阿尔茨海默病抑制剂),表明硫代吗啉杂环可以作为一个重要的药效团,用于开发新型具有药理活性的分子。相信该综述对基于硫代吗啉的药物的开发和合理设计具有重要的新思维意义。