The synthesis and structure-activity relationship of substituted N-phenyl anthranilic acid analogs as amyloid aggregation inhibitors.
It is believed that beta-amyloid aggregation is an important event in the development of Alzheimer's disease. In the course of our studies to identify beta-amyloid aggregation inhibitors, a series of N-phenyl anthranilic acid analogs were synthesized and studied for beta-amyloid inhibition activity. The synthesis, structure-activity relationship, and in vivo activity of these analogs are discussed.
Simons
Lloyd J
LJ
Pfizer Global Research and Development, Ann Arbor Laboratories, 2800 Plymouth Rd., Ann Arbor, MI 48105, USA.
Caprathe
Bradley W
BW
Callahan
Michael
M
Graham
James M
JM
Kimura
Takenori
T
Lai
Yingjie
Y
LeVine
Harry
H
Lipinski
William
W
Sakkab
Annette T
AT
Tasaki
Yoshikazu
Y
Walker
Lary C
LC
Yasunaga
Tomoyuki
T
Ye
Yuyang
Y
Zhuang
Nian
N
Augelli-Szafran
Corinne E
CE
D000544:Alzheimer Disease; D000682:Amyloid / Q000737:chemistry*; D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D004195:Disease Models, Animal; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000494:pharmacology; D054361:Fenamates / Q000138:chemical synthesis / Q000737:chemistry*; D006801:Humans; D051379:Mice; D018625:Microscopy, Atomic Force; D008956:Models, Chemical; D015394:Molecular Structure; D010455:Peptides / Q000737:chemistry; D013329:Structure-Activity Relationship
D000682:Amyloid; D004791:Enzyme Inhibitors; D054361:Fenamates; D010455:Peptides