Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds,Journal of Medicinal Chemistry

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Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2017-11-01 00:00:00 , DOI: 10.1021/acs.jmedchem.7b00718
Remya Ramesh _{1,

2} , D. Srinivasa Reddy _{1,

2}

Affiliation

In order to optimize a lead molecule for further development, bioisosteric replacements are generally adopted as one of the strategies. Silicon appears to be the right choice as a carbon isostere because of the similarity in chemical properties. Silicon can be strategically introduced in a molecule to modulate its druglike properties, providing medicinal chemists with an unconventional strategy for replacing a carbon atom. Silicon can also be introduced to replace other heteroatoms and can act as a surrogate of functional groups such as olefin and amide as well. The present Perspective focuses on the opportunities that silicon incorporation offers in drug discovery, with an emphasis on case studies where introduction of silicon has created a benefit over its analog. We have tried to highlight all the recent developments in the field and briefly discuss the challenges associated with them.

中文翻译：

通过在药物支架中掺入硅来寻求新型化学实体

为了优化用于进一步开发的先导分子，生物等位取代通常被采用作为策略之一。由于化学性质的相似性，硅似乎是碳等排烃的正确选择。硅可以策略性地引入分子中以调节其类药物特性，从而为药物化学家提供了一种替代碳原子的非常规策略。还可以引入硅来代替其他杂原子，并且硅还可以充当官能团（例如烯烃和酰胺）的替代物。本“观点”重点关注硅掺入为药物发现提供的机会，并着重于案例研究，在这些案例中，硅的引入已为其模拟产品带来了收益。

更新日期：2017-11-01

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