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Exploiting the Indole Scaffold to Design Compounds Binding to Different Pharmacological Targets.
- Source :
-
Molecules (Basel, Switzerland) [Molecules] 2020 May 16; Vol. 25 (10). Date of Electronic Publication: 2020 May 16. - Publication Year :
- 2020
-
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 <subscript>A</subscript> ) chloride channel, the translocator protein (TSPO), the murine double minute 2 (MDM2) protein, the A <subscript>2B</subscript> adenosine receptor (A <subscript>2B</subscript> 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.
- 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
Subjects
Details
- Language :
- English
- ISSN :
- 1420-3049
- Volume :
- 25
- Issue :
- 10
- Database :
- MEDLINE
- Journal :
- Molecules (Basel, Switzerland)
- Publication Type :
- Academic Journal
- Accession number :
- 32429433
- Full Text :
- https://doi.org/10.3390/molecules25102331