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Design and optimization of tricyclic gamma-secretase modulators
- Source :
- Bioorganic & Medicinal Chemistry Letters. 26:1498-1502
- Publication Year :
- 2016
- Publisher :
- Elsevier BV, 2016.
-
Abstract
- Beginning with a diaminotriazine screening hit, several series of novel, tricyclic gamma-secretase modulators (GSMs) were designed. The SAR of several related series of GSMs is presented, and the in vivo profile of a lead molecule from the series is described.
- Subjects :
- Stereochemistry
Clinical Biochemistry
Pharmaceutical Science
macromolecular substances
01 natural sciences
Biochemistry
Mice
Structure-Activity Relationship
03 medical and health sciences
0302 clinical medicine
Drug Discovery
Animals
Humans
Protease Inhibitors
Molecular Biology
Gamma secretase
chemistry.chemical_classification
Aniline Compounds
Dose-Response Relationship, Drug
Molecular Structure
biology
Triazines
Chemistry
musculoskeletal, neural, and ocular physiology
Organic Chemistry
Combinatorial chemistry
0104 chemical sciences
010404 medicinal & biomolecular chemistry
nervous system
Drug Design
biology.protein
Molecular Medicine
Amyloid Precursor Protein Secretases
Amyloid precursor protein secretase
030217 neurology & neurosurgery
Tricyclic
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 26
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....f8f1d06820995a17ae709ff042345cc6
- Full Text :
- https://doi.org/10.1016/j.bmcl.2015.06.020