1428443-87-1Relevant academic research and scientific papers
Design and synthesis of a novel series of orally active, selective somatostatin receptor 2 agonists for the treatment of type 2 diabetes
Banno, Yoshihiro,Sasaki, Shigekazu,Kamata, Makoto,Kunitomo, Jun,Miyamoto, Yasufumi,Abe, Hidenori,Taya, Naohiro,Oi, Satoru,Watanabe, Masanori,Urushibara, Tomoko,Hazama, Masatoshi,Niwa, Shin-ichi,Miyamoto, Saku,Horinouchi, Akira,Kuroshima, Ken-ichi,Amano, Nobuyuki,Matsumoto, Shin-ichi,Matsunaga, Shinichiro
, p. 5995 - 6006 (2017/10/10)
The discovery of a novel series of β-methyltryptophan (β MeTrp) derivatives as selective and orally active non-peptide somatostatin receptor 2 (SSTR2) agonists for the treatment of Type 2 diabetes is described. In our previous research, Compound A, β-MeTr
3-Substituted 2-phenyl-indoles: Privileged structures for medicinal chemistry
Johansson, Henrik,Jorgensen, Tanja Bogeloov,Gloriam, David E.,Braeuner-Osborne, Hans,Pedersen, Daniel Sejer
, p. 945 - 960 (2013/04/24)
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.
