title: The synthesis and structure-activity relationship of substituted N-phenyl anthranilic acid analogs as amyloid aggregation inhibitors.
abstract: 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.
authors.affiliation: Pfizer Global Research and Development, Ann Arbor Laboratories, 2800 Plymouth Rd., Ann Arbor, MI 48105, USA.
authors.forename: Lloyd J
authors.initials: LJ
authors.lastname: Simons
authors.forename: Bradley W
authors.initials: BW
authors.lastname: Caprathe
authors.forename: Michael
authors.initials: M
authors.lastname: Callahan
authors.forename: James M
authors.initials: JM
authors.lastname: Graham
authors.forename: Takenori
authors.initials: T
authors.lastname: Kimura
authors.forename: Yingjie
authors.initials: Y
authors.lastname: Lai
authors.forename: Harry
authors.initials: H
authors.lastname: LeVine
authors.forename: William
authors.initials: W
authors.lastname: Lipinski
authors.forename: Annette T
authors.initials: AT
authors.lastname: Sakkab
authors.forename: Yoshikazu
authors.initials: Y
authors.lastname: Tasaki
authors.forename: Lary C
authors.initials: LC
authors.lastname: Walker
authors.forename: Tomoyuki
authors.initials: T
authors.lastname: Yasunaga
authors.forename: Yuyang
authors.initials: Y
authors.lastname: Ye
authors.forename: Nian
authors.initials: N
authors.lastname: Zhuang
authors.forename: Corinne E
authors.initials: CE
authors.lastname: Augelli-Szafran
mesh_terms: 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
chemical_list: D000682:Amyloid; D004791:Enzyme Inhibitors; D054361:Fenamates; D010455:Peptides