Chun, Young Shin Lim, Soo Jeong Oh, Seung Jun Moon, Dae Hyuk Kim, Dong Jin Cho, Cheon-Gyu Yoo, Kyung Ho 2024-01-20T22:34:50Z 2024-01-20T22:34:50Z 2021-09-03 2008-09-20 0253-2964 https://pubs.kist.re.kr/handle/201004/133145 Functionalized benzoxazole derivatives were designed and synthesized based on the structural features of PIB and FDDNP, which show excellent binding affinities to aggregated A beta 42 fibrils. All the synthesized compounds were evaluated by competitive binding assay against aggregated A beta 42 fibrils using [I-125]TZDM and displayed good in vitro binding affinities with K-i values (0.47-15.3 nM) from subnanomolar to nanomolar range. Among them, benzoxazoles 1f and 1a having malononitrile and ester moieties at C-6 exhibited superior binding affinities (K-i = 0.47 and 0.61 nM, respectively) to PIB (K-i = 0.77 nM). English WILEY-V C H VERLAG GMBH BETA-AMYLOID PLAQUES ALZHEIMERS-DISEASE DERIVATIVES PROTEIN AGENTS Synthesis of Functionalized Benzoxazoles and Their Binding Affinities to A beta 42 Fibrils Article 1 BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.29, no.9, pp.1765 - 1768 BULLETIN OF THE KOREAN CHEMICAL SOCIETY 29 9 1765 1768 scie scopus kci ART001525253 000261447200028 2-s2.0-52749091376 Chemistry, Multidisciplinary Chemistry Article BETA-AMYLOID PLAQUES ALZHEIMERS-DISEASE DERIVATIVES PROTEIN AGENTS Alzheimer&apos s disease A beta 42 fibrils Functionalized benzoxazoles Binding affinity