Discovery of 2,4,6-trisubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors.
Development of cis-2,4,6-trisubstituted piperidine N-arylsulfonamides as gamma-secretase inhibitors for the potential treatment of Alzheimer's disease (AD) is reported.
Li
Hongmei
H
Department of Chemical Research, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. hongmei.li@spcorp.cpm
Asberom
Theodros
T
Bara
Thomas A
TA
Clader
John W
JW
Greenlee
William J
WJ
Josien
Hubert B
HB
McBriar
Mark D
MD
Nomeir
Amin
A
Pissarnitski
Dmitri A
DA
Rajagopalan
Murali
M
Xu
Ruo
R
Zhao
Zhiqiang
Z
Song
Lixin
L
Zhang
Lili
L
D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors*; D051544:Cytochrome P-450 CYP3A / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry
D004791:Enzyme Inhibitors; D010880:Piperidines; D013449:Sulfonamides; D051544:Cytochrome P-450 CYP3A; C510163:CYP3A4 protein, human; D053829:Amyloid Precursor Protein Secretases