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8-Fluoroimidazo[1,2-a]pyridine: Synthesis, physicochemical properties and evaluation as a bioisosteric replacement for imidazo[1,2-a]pyrimidine in an allosteric modulator ligand of the GABAA receptor
- Source :
- Bioorganic & Medicinal Chemistry Letters. 16:1518-1522
- Publication Year :
- 2006
- Publisher :
- Elsevier BV, 2006.
-
Abstract
- 8-Fluoroimidazo[1,2-a]pyridine has been established as a physicochemical mimic of imidazo[1,2-a]pyrimidine, using both in silico and traditional techniques. Furthermore, a novel synthesis of a 3,7-disubstituted-8-fluoroimidazopyridine 3 has been developed and the utility of the physicochemical mimicry has been demonstrated in an in vitro system. Here, the 8-fluoroimidazopyridine ring contained in ligand 3 acts as a bioisosteric replacement for imidazopyrimidine in the GABAA receptor modulator 2.
- Subjects :
- Imidazopyridine
Allosteric modulator
Pyrimidine
Pyridines
Stereochemistry
Clinical Biochemistry
Allosteric regulation
Pharmaceutical Science
Ligands
Biochemistry
Chemical synthesis
Mice
Structure-Activity Relationship
chemistry.chemical_compound
Allosteric Regulation
Drug Discovery
Animals
Humans
GABA-A Receptor Agonists
GABA Agonists
Molecular Biology
Molecular Structure
GABAA receptor
Organic Chemistry
Imidazoles
Fibroblasts
Ligand (biochemistry)
Recombinant Proteins
chemistry
Molecular Medicine
Bioisostere
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 16
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....ef699f532ab3641ad2926a675b84cab8