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Exploiting the Indole Scaffold to Design Compounds Binding to Different Pharmacological Targets.

Sabrina TalianiFederico Da SettimoClaudia MartiniSonia LaneriEttore NovellinoGiovanni Greco
Published in: Molecules (Basel, Switzerland) (2020)
Several indole derivatives have been disclosed by our research groups that have been collaborating for nearly 25 years. The results of our investigations led to a variety of molecules binding selectively to different pharmacological targets, specifically the type A γ-aminobutyric acid (GABAA) chloride channel, the translocator protein (TSPO), the murine double minute 2 (MDM2) protein, the A2B adenosine receptor (A2B AR) and the Kelch-like ECH-associated protein 1 (Keap1). Herein, we describe how these works were conceived and carried out thanks to the versatility of indole nucleus to be exploited in the design and synthesis of drug-like molecules.
Keyphrases
  • protein protein
  • binding protein
  • amino acid
  • small molecule
  • emergency department
  • computed tomography
  • protein kinase
  • pet imaging
  • drug induced
  • electronic health record