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Discovery of sulfonamide-pyrazole gamma-secretase inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Apr 01; Vol. 20 (7), pp. 2148-50. Date of Electronic Publication: 2010 Feb 14. - Publication Year :
- 2010
-
Abstract
- Utilizing a pharmacophore hypothesis, previously described gamma-secretase inhibiting HTS hits were evolved into novel tricyclic sulfonamide-pyrazoles, with high in vitro potency, good brain penetration, low metabolic stability, and high clearance.<br /> (2010 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Crystallography, X-Ray
Humans
Inhibitory Concentration 50
Models, Molecular
Pyrazoles chemistry
Pyrazoles pharmacokinetics
Rats
Rats, Sprague-Dawley
Structure-Activity Relationship
Sulfonamides chemistry
Sulfonamides pharmacokinetics
Alzheimer Disease drug therapy
Amyloid Precursor Protein Secretases antagonists & inhibitors
Amyloid Precursor Protein Secretases metabolism
Pyrazoles pharmacology
Sulfonamides pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 20
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 20206516
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.02.050