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基于1,1-二取代-1-硅杂环烷的化合物库的设计与合成。

Design and synthesis of 1,1-disubstituted-1-silacycloalkane-based compound libraries.

作者信息

Ortega Raquel, Sanchez-Quesada Jorge, Lorenz Christoph, Dolega Grzegorg, Karawajczyk Anna, Sanz Miguel, Showell Graham, Giordanetto Fabrizio

机构信息

Medicinal Chemistry, Taros Chemicals GmbH & Co. KG, Emil-Figge-Str. 76a, 44227 Dortmund, Germany.

Medicinal Chemistry, Taros Chemicals GmbH & Co. KG, Emil-Figge-Str. 76a, 44227 Dortmund, Germany.

出版信息

Bioorg Med Chem. 2015 Jun 1;23(11):2716-20. doi: 10.1016/j.bmc.2015.01.046. Epub 2015 Feb 3.

Abstract

The introduction of silicon in biologically-relevant molecules represents an interesting medicinal chemistry tactic. Its use is mainly confined to the fine-tuning of specific molecular properties and organosilicon compounds are underrepresented in typical screening libraries. As part of the European Lead Factory efforts to generate novel, drug discovery-relevant chemical matter, the design and synthesis of 1,1-disubstituted-1-silacycloalkane-based compound libraries is described.

摘要

在具有生物学相关性的分子中引入硅是一种有趣的药物化学策略。其应用主要局限于特定分子性质的微调,且有机硅化合物在典型的筛选文库中占比不足。作为欧洲先导化合物工厂致力于生成新型、与药物发现相关化学物质的一部分,本文描述了基于1,1-二取代-1-硅杂环烷的化合物文库的设计与合成。

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