Evolution of tertiary carbinamine BACE-1 inhibitors: Abeta reduction in rhesus CSF upon oral dosing.
Nantermet
Philippe G
PG
Department of Medicinal Chemistry, Merck Research Laboratories, P.O Box 4, WP14-3, West Point, PA 19486, USA. philippe_nantermet@merck.com
Rajapakse
Hemaka A
HA
Stanton
Mathew G
MG
Stauffer
Shaun R
SR
Barrow
James C
JC
Gregro
Allison R
AR
Moore
Keith P
KP
Steinbeiser
Melissa A
MA
Swestock
John
J
Selnick
Harold G
HG
Graham
Samuel L
SL
McGaughey
Georgia B
GB
Colussi
Dennis
D
Lai
Ming-Tain
MT
Sankaranarayanan
Sethu
S
Simon
Adam J
AJ
Munshi
Sanjeev
S
Cook
Jacquelynn J
JJ
Holahan
Marie A
MA
Michener
Maria S
MS
Vacca
Joseph P
JP
D000284:Administration, Oral; D000588:Amines / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D016229:Amyloid beta-Peptides / Q000134:cerebrospinal fluid*; D000818:Animals; D001812:Blood-Brain Barrier; D018360:Crystallography, X-Ray; D000882:Haplorhini; D020128:Inhibitory Concentration 50; D008253:Macaca mulatta; D008968:Molecular Conformation; D010446:Peptide Fragments / Q000134:cerebrospinal fluid*; D011480:Protease Inhibitors / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000588:Amines; D016229:Amyloid beta-Peptides; D010446:Peptide Fragments; D011480:Protease Inhibitors; C538897:amyloid beta-protein (40-42); D053829:Amyloid Precursor Protein Secretases