Vandekerckhove Stéphanie, D'hooghe Matthias
SynBioC Research Group, Department of Sustainable Organic Chemistry and Technology, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, B-9000 Ghent, Belgium.
SynBioC Research Group, Department of Sustainable Organic Chemistry and Technology, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, B-9000 Ghent, Belgium.
Bioorg Med Chem. 2015 Aug 15;23(16):5098-119. doi: 10.1016/j.bmc.2014.12.018. Epub 2014 Dec 19.
Quinoline-containing compounds, such as quinine and chloroquine, have a long-standing history as potent antimalarial agents. However, the increasing resistance of the Plasmodium parasite against these drugs and the lack of licensed malaria vaccines have forced chemists to develop synthetic strategies toward novel biologically active molecules. A strategy that has attracted considerable attention in current medicinal chemistry is based on the conjugation of two biologically active molecules into one hybrid compound. Since quinolines are considered to be privileged antimalarial building blocks, the synthesis of quinoline-containing antimalarial hybrids has been elaborated extensively in recent years. This review provides a literature overview of antimalarial hybrid molecules containing a quinoline core, covering publications between 2009 and 2014.
含喹啉的化合物，如奎宁和氯喹，作为有效的抗疟药物有着悠久的历史。然而，疟原虫对这些药物的耐药性不断增加，且缺乏获得许可的疟疾疫苗，这迫使化学家们开发针对新型生物活性分子的合成策略。当前药物化学中一个备受关注的策略是将两个生物活性分子共轭成一个杂合化合物。由于喹啉被认为是具有优势的抗疟结构单元，近年来含喹啉抗疟杂合物的合成得到了广泛的研究。本综述提供了含喹啉核心的抗疟杂合分子的文献概述，涵盖了2009年至2014年期间的出版物。
