1. Exploiting the Indole Scaffold to Design Compounds Binding to Different Pharmacological Targets.
- Author
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Taliani S, Da Settimo F, Martini C, Laneri S, Novellino E, and Greco G
- Subjects
- Animals, Diazepam pharmacology, GABA Modulators pharmacology, Humans, Indoles pharmacology, Kelch-Like ECH-Associated Protein 1 agonists, Kelch-Like ECH-Associated Protein 1 antagonists & inhibitors, Kelch-Like ECH-Associated Protein 1 metabolism, Ligands, Mice, Protein Binding, Proto-Oncogene Proteins c-mdm2 antagonists & inhibitors, Proto-Oncogene Proteins c-mdm2 chemistry, Proto-Oncogene Proteins c-mdm2 metabolism, Receptor, Adenosine A2B chemistry, Receptor, Adenosine A2B metabolism, Receptors, GABA chemistry, Receptors, GABA metabolism, Receptors, GABA-A chemistry, Structure-Activity Relationship, Diazepam analogs & derivatives, Drug Design, GABA Modulators chemical synthesis, Indoles chemical synthesis, Receptors, GABA-A metabolism
- Abstract
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 (GABA
A ) 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.- Published
- 2020
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