3-Substituted 2-phenyl-indoles: Privileged structures for medicinal chemistry
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.
Johansson, Henrik,Jorgensen, Tanja Bogeloov,Gloriam, David E.,Braeuner-Osborne, Hans,Pedersen, Daniel Sejer
p. 945 - 960
(2013/04/24)
Diphenylbutyl-1-acylpiperazines
Novel compounds of the formula STR1 wherein R' is selected from the group consisting of alkyl straight or branch chained having from 2 to 10 carbon atoms, cycloalkyl having from 3 to 8 carbon atoms, aralkyl having from 7 to 9 carbon atoms, phenyl and subs
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(2008/06/13)
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