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

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

doi:10.1016/j.bmc.2015.01.046

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

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

Authors

Raquel Ortega¹, Jorge Sanchez-Quesada¹, Christoph Lorenz¹, Grzegorg Dolega¹, Anna Karawajczyk¹, Miguel Sanz¹, Graham Showell¹, Fabrizio Giordanetto²

Affiliations

¹ Medicinal Chemistry, Taros Chemicals GmbH & Co. KG, Emil-Figge-Str. 76a, 44227 Dortmund, Germany.
² Medicinal Chemistry, Taros Chemicals GmbH & Co. KG, Emil-Figge-Str. 76a, 44227 Dortmund, Germany. Electronic address: fgiordanetto@tarosdiscovery.com.

PMID: 25680845
DOI: 10.1016/j.bmc.2015.01.046

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.

Keywords: Bioisostere; Silacycloalkane; Silacyclohexane; Silacyclopentane; Silicon.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Drug Design*
Drug Discovery*
Molecular Structure
Organosilicon Compounds / chemical synthesis*
Small Molecule Libraries / chemical synthesis*

Substances

Organosilicon Compounds
Small Molecule Libraries