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Bridging free radical chemistry with drug discovery: A promising way for finding novel drugs efficiently.
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2019-12-30 , DOI: 10.1016/j.ejmech.2019.112020
Zai-Qun Liu 1
Affiliation  

Many diseases have been regarded to correlate with the in vivo oxidative damages, which are caused by overproduced free radicals from metabolic process or reactive oxygen species (ROS). This background motivates chemists to explore free radical reactions and to design a number of antioxidants, but whether free radical chemistry can be applied to accelerate the efficacy of the drug discovery is still underrepresented. Herein, in light of recent findings as well as kinetics on free radical reaction, the discipline of free radical chemistry is introduced to be a novel tool for finding potential drugs from antioxidant libraries accumulated during the study on free radical chemistry. These antioxidants provide with such abundant types of structural skeleton that might be employed to inhibit oxidations in different biological microenvironments. Although the in vitro characterization on the antioxidative property exerts a potential role of an antioxidant as a prodrug, the in vivo investigation on the property for quenching free radicals will make a final decision for the antioxidant whether it is worthy to be further explored pharmacologically. Therefore, it is reasonable to expect that bridging free radical chemistry with the pharmacological research will provide with a succinct way for finding novel drugs efficiently.

中文翻译:

将自由基化学与药物发现联系起来:一种有效地寻找新药物的有前途的方法。

许多疾病被认为与体内氧化损伤有关,这是由于代谢过程或活性氧(ROS)产生的自由基过多而引起的。这种背景促使化学家们探索自由基反应并设计许多抗氧化剂,但是自由基化学是否可用于加速药物发现的功效仍然未被充分描述。在此,根据最近的发现以及自由基反应的动力学,引入自由基化学学科作为从自由基化学研究期间积累的抗氧化剂库中寻找潜在药物的新颖工具。这些抗氧化剂具有如此丰富的结构骨架类型,可用于抑制不同生物微环境中的氧化。尽管抗氧化特性的体外表征发挥了抗氧化剂作为前药的潜在作用,但体内对自由基猝灭特性的研究将最终决定抗氧化剂是否值得在药理上进一步探索。因此,有理由期望将自由基化学与药理学研究联系起来将为有效地发现新药提供一种简洁的方法。
更新日期:2019-12-30
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