title: Ferulic acid and benzothiazole dimer derivatives with high binding affinity to beta-amyloid fibrils.
abstract: New ferulic acid and benzothiazole dimer derivatives were synthesized and evaluated by in vitro competition assay using [(125)I]TZDM for their specific binding affinities to Abeta fibrils. In particular, 4a showed the most excellent binding affinity (K(i)=0.53 nM), compared to PIB (K(i)=0.77 nM), for benzothiazole binding sites of Abeta(1-42) fibrils. This result suggests a possibility of a potential AD diagnostic probe for detection of Abeta fibrils.
authors.affiliation: Center for Chemoinformatics Research, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, South Korea.
authors.forename: Seong Rim
authors.initials: SR
authors.lastname: Byeon
authors.forename: Yun Jung
authors.initials: YJ
authors.lastname: Jin
authors.forename: Soo Jeong
authors.initials: SJ
authors.lastname: Lim
authors.forename: Ji Hoon
authors.initials: JH
authors.lastname: Lee
authors.forename: Kyung Ho
authors.initials: KH
authors.lastname: Yoo
authors.forename: Kye Jung
authors.initials: KJ
authors.lastname: Shin
authors.forename: Seung Jun
authors.initials: SJ
authors.lastname: Oh
authors.forename: Dong Jin
authors.initials: DJ
authors.lastname: Kim
mesh_terms: D016229:Amyloid beta-Peptides / Q000378:metabolism*; D052160:Benzothiazoles / Q000737:chemistry / Q000378:metabolism*; D003373:Coumaric Acids / Q000737:chemistry / Q000378:metabolism*; D019281:Dimerization; D013329:Structure-Activity Relationship
chemical_list: D016229:Amyloid beta-Peptides; D052160:Benzothiazoles; D003373:Coumaric Acids; C004999:ferulic acid