苯胺等排体替代的最新进展与展望
Recent Advances and Outlook for the Isosteric Replacement of Anilines.
作者信息
Sodano Taylor M, Combee Logan A, Stephenson Corey R J
机构信息
Department of Chemistry, University of Michigan, Ann Arbor, Michigan 48109, United States.
出版信息
ACS Med Chem Lett. 2020 Feb 21;11(10):1785-1788. doi: 10.1021/acsmedchemlett.9b00687. eCollection 2020 Oct 8.
Abstract
Many promising drug candidates and pharmaceutical compounds fail due to idiosyncratic adverse drug reactions (IADRs), often arising from the formation of reactive metabolites. Among the "structural alerts" responsible, anilines are well-known to undergo deleterious metabolic processing, yet isosteric replacement strategies remain limited. Herein we discuss current art and potential new avenues of saturated isosteres to mitigate aniline-related toxicities.
摘要
许多有前景的候选药物和药物化合物因特异质药物不良反应（IADR）而失败，这些反应通常源于活性代谢物的形成。在造成这种情况的“结构警示”中，苯胺因会经历有害的代谢过程而广为人知，但等排体替代策略仍然有限。在此，我们讨论目前关于饱和等排体以减轻苯胺相关毒性的技术水平和潜在新途径。
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