@article{oai:nagasaki-u.repo.nii.ac.jp:00015665, author = {Watanabe, Hiroyuki and Ono, Masahiro and Ikeoka, Ryoichi and Haratake, Mamoru and Saji, Hideo and Nakayama, Morio}, issue = {17}, journal = {Bioorganic & medicinal chemistry}, month = {Sep}, note = {This paper describes the synthesis and biological evaluation of a new series of 2,5-diphenyl-1,3,4-oxadiazole (1,3,4-DPOD) derivatives for detecting beta-amyloid plaques in Alzheimer's brains. The affinity for beta-amyloid plaques was assessed by an in vitro binding assay using pre-formed synthetic Abeta42 aggregates. The new series of 1,3,4-DPOD derivatives showed affinity for Abeta42 aggregates with K(i) values ranging from 20 to 349 nM. The 1,3,4-DPOD derivatives clearly stained beta-amyloid plaques in an animal model of Alzheimer's disease, reflecting the affinity for Abeta42 aggregates in vitro. Compared to 3,5-diphenyl-1,2,4-oxadiazole (1,2,4-DPOD) derivatives, they displayed good penetration of and fast washout from the brain in biodistribution experiments using normal mice. The novel radioiodinated 1,3,4-DPOD derivatives may be useful probes for detecting beta-amyloid plaques in the Alzheimer's brain., Bioorganic & medicinal chemistry, 17(17), pp.6402-6406; 2009}, pages = {6402--6406}, title = {Synthesis and biological evaluation of radioiodinated 2,5-diphenyl-1,3,4-oxadiazoles for detecting beta-amyloid plaques in the brain.}, volume = {17}, year = {2009} }