Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Sector 67, S.A.S. Nagar, Punjab 160 062, India.
Eur J Med Chem. 2010 Aug;45(8):3245-64. doi: 10.1016/j.ejmech.2010.04.011. Epub 2010 Apr 18.
The quinoline scaffold is prevalent in a variety of pharmacologically active synthetic and natural compounds. The discovery of chloroquine, the most famous drug containing this scaffold resulted in control and eradication of malaria for decades. The other known antimalarial drugs from the quinoline family include: quinine, amodiaquine, piperaquine, primaquine, and mefloquine. The drugs from this group mostly act during the blood stages of the parasite's life cycle but some like primaquine targets the tissue stages. This review provides a comprehensive literature compilation concerning the study of quinolines and also other heterocycles structurally similar to quinoline scaffold in the treatment of malaria. This review covers advances made in the last ten years and it is subdivided into eight sub-headings. It consists of discussion on the biological activities, structure-activity relationship, and potential biochemical pathways of 4-aminoquinolines, 4-anilinoquinolines, 8-aminoquinolines, quinolines from nature, quinolones, isoquinolines and tetrahydroquinolines, ring-modified quinolines, and miscellaneous quinolines.
喹啉骨架广泛存在于各种具有药理活性的合成和天然化合物中。氯喹是该骨架中最著名的药物,它的发现使得疟疾在几十年内得到了控制和根除。喹啉类家族的其他已知抗疟药物包括:奎宁、阿莫地喹、哌喹、伯氨喹和甲氟喹。该类药物主要在寄生虫生命周期的血液阶段发挥作用,但有些药物,如伯氨喹,针对组织阶段。本综述提供了关于喹啉及其与喹啉骨架结构相似的其他杂环化合物在治疗疟疾方面的研究的全面文献汇编。本综述涵盖了过去十年的进展,分为八个小标题。它包括对 4-氨基喹啉、4-苯胺基喹啉、8-氨基喹啉、天然喹啉、喹诺酮、异喹啉和四氢喹啉、环修饰喹啉和杂环喹啉的生物活性、构效关系和潜在生化途径的讨论。