Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.,Journal of Medicinal Chemistry

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Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2020-09-11 , DOI: 10.1021/acs.jmedchem.0c01177
Christian Gampe ₁ , Vishal A Verma ₁

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There is a dichotomy between the increasing utility of aldehydes as tool molecules that bind to “undruggable” protein sites and the designation of the aldehyde functional group as a structural alert by the medicinal chemistry community. Herein we compile information about pharmacologically active aldehydes that are being used in humans. We summarize the learnings from these data, discuss advantages and challenges associated with aldehydes, and derive strategies for the successful development of aldehydes within drug discovery programs.

中文翻译：

诅咒还是治愈？醛作为活性药物成分的可开发性透视。

在醛作为与“不可吸收的”蛋白质位点结合的工具分子的效用增加与醛官能团被医学化学界指定为结构性警戒之间存在分歧。在这里，我们汇总了有关在人类中使用的药理活性醛的信息。我们总结了这些数据的学习成果，讨论了与醛相关的优势和挑战，并提出了在药物发现计划中成功开发醛的策略。

更新日期：2020-09-11

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