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Exploiting the Indole Scaffold to Design Compounds Binding to Different Pharmacological Targets
- Source :
- Molecules, Molecules, Vol 25, Iss 2331, p 2331 (2020)
- Publication Year :
- 2020
- Publisher :
- MDPI AG, 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 (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.
- Subjects :
- Indoles
Pharmaceutical Science
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)
Review
Ligands
01 natural sciences
Analytical Chemistry
Mice
Murine double Minute 2 (MDM2) protein
Drug Discovery
0303 health sciences
Kelch-Like ECH-Associated Protein 1
biology
Chemistry
GABAA receptor
Proto-Oncogene Proteins c-mdm2
Chemistry (miscellaneous)
A2B adenosine receptor (A2B AR)
Chloride channel
Molecular Medicine
Mdm2
Protein Binding
Stereochemistry
Translocator protein (TSPO)
type A γ-aminobutyric acid (GABAA) chloride channel
Receptor, Adenosine A2B
lcsh:QD241-441
Structure-Activity Relationship
03 medical and health sciences
lcsh:Organic chemistry
Receptors, GABA
Translocator protein
Animals
Humans
Kelch-like ECH-associated protein 1 (Keap1)
Molecule
Physical and Theoretical Chemistry
GABA Modulators
030304 developmental biology
Indole test
Diazepam
Organic Chemistry
Receptors, GABA-A
Type A γ-aminobutyric acid (GABAA) chloride channel
KEAP1
Adenosine receptor
0104 chemical sciences
010404 medicinal & biomolecular chemistry
Drug Design
biology.protein
Subjects
Details
- ISSN :
- 14203049
- Volume :
- 25
- Database :
- OpenAIRE
- Journal :
- Molecules
- Accession number :
- edsair.doi.dedup.....3d18b35f73f2b241ee4a009500b83347
- Full Text :
- https://doi.org/10.3390/molecules25102331