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抗疟药物靶向表观遗传学或线粒体：针对疟疾的潜在药物的合成和生物学评价的最新研究进展。

Antimalarial Inhibitors Targeting Epigenetics or Mitochondria in : Recent Survey upon Synthesis and Biological Evaluation of Potential Drugs against Malaria.

机构信息

CNRS, LCC (Laboratoire de Chimie de Coordination), Université de Toulouse, UPS, INPT, Inserm ERL 1289, 205 Route de Narbonne, BP 44099, CEDEX 4, F-31077 Toulouse, France.

Synthetic Organic Chemistry Laboratory, Department of Chemistry, University of Patras, GR-26504 Patras, Greece.

出版信息

Molecules. 2021 Sep 21;26(18):5711. doi: 10.3390/molecules26185711.

DOI:10.3390/molecules26185711
PMID:34577183
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8467436/
Abstract

Despite many efforts, malaria remains among the most problematic infectious diseases worldwide, mainly due to the development of drug resistance by Over the past decade, new essential pathways have been emerged to fight against malaria. Among them, epigenetic processes and mitochondrial metabolism appear to be important targets. This review will focus on recent evolutions concerning worldwide efforts to conceive, synthesize and evaluate new drug candidates interfering selectively and efficiently with these two targets and pathways. The focus will be on compounds/scaffolds that possess biological/pharmacophoric properties on DNA methyltransferases and HDAC's for epigenetics, and on cytochrome bc1 and dihydroorotate dehydrogenase for mitochondrion.

摘要

尽管付出了许多努力，疟疾仍然是全球最具问题的传染病之一，主要是由于耐药性的出现。在过去的十年中，出现了新的基本途径来对抗疟疾。其中，表观遗传过程和线粒体代谢似乎是重要的靶点。这篇综述将集中讨论近年来在构思、合成和评估新的候选药物方面的全球努力，这些药物能够选择性和有效地干扰这两个靶点和途径。重点将放在具有 DNA 甲基转移酶和组蛋白去乙酰化酶表观遗传生物/药效性质的化合物/支架，以及细胞色素 bc1 和二氢乳清酸脱氢酶的化合物/支架上。

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