Journal
RSC ADVANCES
Volume 3, Issue 3, Pages 945-960Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c2ra21902f
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Funding
- Faculty of Health and Medical Sciences, University of Copenhagen
- Danish Council for Independent Research, Medical Sciences
- Lundbeck Foundation
- Drug Research Academy, Faculty of Health and Medical Sciences, University of Copenhagen
- Alfred Benzon Foundation
- Carlsberg Foundation
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Privileged structures have been used in drug discovery targeting G protein-coupled receptors ( GPCR) and other protein classes for more than 20 years. Their rich activity profiles and drug-like characteristics lend themselves to increased productivity in hit identification and lead optimisation. Recently we discovered two allosteric modulators 1 and 2 for the G protein-coupled receptor GPRC6A incorporating the privileged 2-phenyl-indole scaffold, functionalised at the 3-position. In order to develop new potential GPRC6A ligands we engaged in the development of synthetic routes to provide 2-phenyl-indoles with a variety of substituents at the indole 3-position. Herein we describe the development of optimised and efficient synthetic routes to a series of new 2-phenyl-indole building blocks 3 to 9 and show that these can be used to generate a broad variety of 3-substituted 2-phenyl-indoles of interest to medicinal chemists.
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