The identification of novel acid isostere based inhibitors of the VPS10P family sorting receptor Sortilin

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  • Jacob Lauwring Andersen
  • ,
  • Samsa Lindberg, Neuroscience Drug Discovery, H. Lundbeck A/S, Copenhagen, Denmark.
  • ,
  • Morten Langgård, Neuroscience Drug Discovery, H. Lundbeck A/S, Copenhagen, Denmark.
  • ,
  • Philip J Maltas, Neuroscience Drug Discovery, H. Lundbeck A/S, Copenhagen, Denmark.
  • ,
  • Lars Christian Biilmann Rønn, Neuroscience Drug Discovery, H. Lundbeck A/S, Copenhagen, Denmark.
  • ,
  • Christoffer Bundgaard, Neuroscience Drug Discovery, H. Lundbeck A/S, Copenhagen, Denmark.
  • ,
  • Dorthe Strandbygaard
  • Søren Thirup
  • Stephen Paul Watson, Neuroscience Drug Discovery, H- Lundbeck A/S, Copenhagen, Denmark. Electronic address: steve.watson@heptares.com.

Using fragment based and structure based drug discovery strategies a series of novel Sortilin inhibitors has been identified. The inhibitors are based on the N-substituted 1,2,3-triazol-4-one/ol heterocyclic template. X-ray crystallography shows that the 1,2,3-triazol-4-one/ol acts as a carboxylic acid isostere, making a bi-dentate interaction with an arginine residue of Sortilin, an interaction which has not been previously characterised for this heterocycle.

OriginalsprogEngelsk
TidsskriftBioorganic & Medicinal Chemistry Letters
Vol/bind27
Nummer11
Sider (fra-til)2629-2633
Antal sider5
ISSN0960-894X
DOI
StatusUdgivet - 1 jun. 2017

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