Laboratory of Medicinal Chemistry, Institute of Organic Chemistry, CSIC; Juan de la Cierva, 3, 28006 Madrid, Spain.
J Med Chem. 2020 Nov 25;63(22):13413-13427. doi: 10.1021/acs.jmedchem.0c00976. Epub 2020 Sep 18.
The recent advances of tetramethylpyrazine nitrones and quinolylnitrones for the treatment of stroke have been reviewed and compared with other agents, showing promising therapeutic applications. As a result of a functional transformation of natural product ligustrazine, ()--butyl-1-(3,5,6-trimethylpyrazin-2-yl)methanimine oxide () is a multitarget small nitrone showing potent thrombolytic activity and free radicals scavenging power, in addition to nontoxicity and blood-brain barrier permeability. Similarly, antioxidant ()--butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine oxide () is a novel agent for cerebral ischemia therapy as it is able to scavenge different types of free radical species, showing strong neuroprotection and reduced infarct size.
最近，四甲基吡嗪硝酮和喹啉硝酮在治疗中风方面的进展已经被综述，并与其他药物进行了比较，显示出有希望的治疗应用。作为天然产物川芎嗪的一种功能转化，（）-正丁基-1-（3,5,6-三甲基吡嗪-2-基）甲亚胺氧化物（）是一种多靶点的小硝酮，具有很强的溶栓活性和自由基清除能力，同时还具有非毒性和血脑屏障通透性。同样，抗氧化剂（）-正丁基-1-（2-氯-6-甲氧基喹啉-3-基）甲亚胺氧化物（）是一种新型的脑缺血治疗药物，因为它能够清除不同类型的自由基，具有很强的神经保护作用和减小梗死面积。
