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Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Nov 15; Vol. 21 (22), pp. 6909-15. Date of Electronic Publication: 2011 Jul 02. - Publication Year :
- 2011
-
Abstract
- The synthesis, evaluation, and structure-activity relationships of a set of related constrained diaminopropane inhibitors of BACE-1 are described. The full in vivo profile of an optimized inhibitor in both normal and P-gp deficient mice is compared with data generated in normal rats.<br /> (Copyright © 2011 Elsevier Ltd. All rights reserved.)
- Subjects :
- ATP Binding Cassette Transporter, Subfamily B, Member 1 genetics
Alzheimer Disease drug therapy
Animals
Aspartic Acid Endopeptidases antagonists & inhibitors
Aspartic Acid Endopeptidases metabolism
Crystallography, X-Ray
Diamines chemical synthesis
Diamines pharmacokinetics
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors pharmacokinetics
HEK293 Cells
Humans
Mice
Mice, Knockout
Models, Molecular
Rats
Structure-Activity Relationship
Amyloid Precursor Protein Secretases antagonists & inhibitors
Amyloid Precursor Protein Secretases metabolism
Diamines chemistry
Diamines pharmacology
Enzyme Inhibitors chemistry
Enzyme Inhibitors pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 21
- Issue :
- 22
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21974952
- Full Text :
- https://doi.org/10.1016/j.bmcl.2011.06.116