Zhejiang Provincial Engineering Technology Research Center of Marine Biomedical Products, School of Food and Pharmacy, Zhejiang Ocean University, Zhoushan, 316022, PR China.
Guangxi Key Laboratory of Chemistry and Engineering of Forest Products, Key Laboratory of Guangxi Colleges and Universities for Food Safety and Pharmaceutical Analytical Chemistry, School of Chemistry and Chemical Engineering, Guangxi University of Nationalities, Nanning, 530006, PR China.
Eur J Med Chem. 2019 Jan 1;161:101-117. doi: 10.1016/j.ejmech.2018.10.035. Epub 2018 Oct 16.
Quinoline and quinolone motifs which act as structural subunits of more complex natural products are ubiquitous in nature, and they are useful pharmacophores which play a pivotal role in drug development. Compared with the corresponding monomeric compounds, the dimers usually exhibited some unique properties, so dimers have caused great interests in recent years. Quinline and quinolone dimers possess various biological properties such as antibacterial, anticancer, antimalarial and antitubercular activities, and some of them which are exemplified by piperaquine have already used in clinical practice. Numerous quinline and quinolone dimers have been synthesized and screened for their in vitro and in vivo biological activities, and some of them exhibited promising potency. Therefore, quinline and quinolone dimers have the potential for clinical deployment in the control and eradication of various diseases. This review covers the recent advances of quinline and quinolone dimers as bioactive substances. The structure-activity relationship was also discussed to provide an insight for rational designs of more active quinline and quinolone dimers.
喹啉和喹诺酮基元作为更复杂天然产物的结构亚单位在自然界中无处不在，它们是药物开发中发挥关键作用的有用药效团。与相应的单体化合物相比，二聚体通常表现出一些独特的性质，因此近年来引起了极大的兴趣。喹啉和喹诺酮二聚体具有多种生物活性，如抗菌、抗癌、抗疟和抗结核活性，其中一些以哌喹为例已在临床上应用。已经合成了大量的喹啉和喹诺酮二聚体，并对其进行了体外和体内生物活性筛选，其中一些表现出有希望的活性。因此，喹啉和喹诺酮二聚体有可能在控制和消除各种疾病方面进行临床部署。本综述涵盖了作为生物活性物质的喹啉和喹诺酮二聚体的最新进展。还讨论了结构-活性关系，为设计更具活性的喹啉和喹诺酮二聚体提供了深入了解。
