Ferulic acid and benzothiazole dimer derivatives with high binding affinity to beta-amyloid fibrils.
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.
Byeon
Seong Rim
SR
Center for Chemoinformatics Research, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, South Korea.
Jin
Yun Jung
YJ
Lim
Soo Jeong
SJ
Lee
Ji Hoon
JH
Yoo
Kyung Ho
KH
Shin
Kye Jung
KJ
Oh
Seung Jun
SJ
Kim
Dong Jin
DJ
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
D016229:Amyloid beta-Peptides; D052160:Benzothiazoles; D003373:Coumaric Acids; C004999:ferulic acid