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Carba Analogues of Flupirtine and Retigabine with Improved Oxidation Resistance and Reduced Risk of Quinoid Metabolite Formation
ChemMedChem ( IF 3.4 ) Pub Date : 2022-06-10 , DOI: 10.1002/cmdc.202200262
Konrad W Wurm 1 , Frieda-Marie Bartz 1 , Lukas Schulig 1 , Anja Bodtke 1 , Patrick J Bednarski 1 , Andreas Link 1
Affiliation  

With the aim of providing safer replacements for the KV7 potassium channel openers flupirtine and retigabine, the oxidation-sensitive triaminoaryl scaffold was modified in a ligand-based approach in order to obtain oxidation-resistant carba derivatives. Some of these novel analogues have a negligible risk for the formation of quinoid metabolites and possess potent KV7.2/3 opening activity.

中文翻译:

氟吡汀和瑞替加滨的卡巴类似物,具有改善的抗氧化性和降低醌类代谢物形成的风险

为了为 K V 7 钾通道开放剂氟吡汀和瑞替加滨提供更安全的替代品,以基于配体的方法对氧化敏感的三氨基芳基支架进行了修饰,以获得抗氧化的卡巴衍生物。其中一些新型类似物形成醌类代谢物的风险可以忽略不计,并具有有效的 K V 7.2/3 开放活性。
更新日期:2022-06-10
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