Barresi Elisabetta, Robello Marco, Baglini Emma, Poggetti Valeria, Viviano Monica, Salerno Silvia, Da Settimo Federico, Taliani Sabrina
Department of Pharmacy, University of Pisa, Via Bonanno 6, 56126 Pisa, Italy.
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK), National Institutes of Health, 9000 Rockville Pike, Bethesda, MD 20892, USA.
Pharmaceuticals (Basel). 2023 Jul 12;16(7):997. doi: 10.3390/ph16070997.
In recent years, indolylglyoxylamide-based derivatives have received much attention due to their application in drug design and discovery, leading to the development of a wide array of compounds that have shown a variety of pharmacological activities. Combining the indole nucleus, already validated as a "privileged structure," with the glyoxylamide function allowed for an excellent template to be obtained that is suitable to a great number of structural modifications aimed at permitting interaction with specific molecular targets and producing desirable therapeutic effects. The present review provides insight into how medicinal chemists have elegantly exploited the indolylglyoxylamide moiety to obtain potentially useful drugs, with a particular focus on compounds exhibiting activity in in vivo models or reaching clinical trials. All in all, this information provides exciting new perspectives on existing data that can be useful in further design of indolylglyoxylamide-based molecules with interesting pharmacological profiles. The aim of this report is to present an update of collection data dealing with the employment of this moiety in the rational design of compounds that are able to interact with a specific target, referring to the last 20 years.
近年来,基于吲哚基乙二醛酰胺的衍生物因其在药物设计与发现中的应用而备受关注,这促使了大量具有多种药理活性的化合物的开发。将已被确认为“优势结构”的吲哚核与乙二醛酰胺官能团相结合,得到了一个出色的模板,该模板适用于大量旨在与特定分子靶点相互作用并产生理想治疗效果的结构修饰。本综述深入探讨了药物化学家如何巧妙地利用吲哚基乙二醛酰胺部分来获得潜在有用的药物,特别关注在体内模型中表现出活性或进入临床试验的化合物。总而言之,这些信息为现有数据提供了令人兴奋的新视角,有助于进一步设计具有有趣药理特性的基于吲哚基乙二醛酰胺的分子。本报告的目的是呈现过去20年中有关该部分在能够与特定靶点相互作用的化合物的合理设计中的应用的收集数据的更新情况。