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Thiophene substituted acylguanidines as BACE1 inhibitors
- Source :
- Bioorganic & Medicinal Chemistry Letters. 17:5353-5356
- Publication Year :
- 2007
- Publisher :
- Elsevier BV, 2007.
-
Abstract
- A series of thiophene-substituted acylguanidines were designed from a pyrrole substituted acylguanidine HTS lead. This template allowed a greater flexibility, through differential Suzuki couplings, to explore the binding site of BACE1 and to enhance the inhibitory potencies. This exploration provided a 25-fold enhancement in potency to yield compound 10a, which was 150 nM in a BACE1 FRET assay.
- Subjects :
- Models, Molecular
Molecular model
Stereochemistry
Clinical Biochemistry
Pharmaceutical Science
Ether
Thiophenes
Crystallography, X-Ray
Guanidines
Biochemistry
Chemical synthesis
Structure-Activity Relationship
chemistry.chemical_compound
mental disorders
Drug Discovery
Hydrolase
Thiophene
Aspartic Acid Endopeptidases
Pyrroles
Enzyme Inhibitors
Binding site
Molecular Biology
Pyrrole
Organic Chemistry
Förster resonance energy transfer
chemistry
Drug Design
Molecular Medicine
Indicators and Reagents
Amyloid Precursor Protein Secretases
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 17
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....bc4b3dd8fc11b23029f7bcb83b6b9caa