Synthesis of Functionalized Benzoxazoles and Their Binding Affinities to A beta 42 Fibrilsopen access
- Authors
- Chun, Young Shin; Lim, Soo Jeong; Oh, Seung Jun; Moon, Dae Hyuk; Kim, Dong Jin; Cho, Cheon-Gyu; Yoo, Kyung Ho
- Issue Date
- Sep-2008
- Publisher
- WILEY-V C H VERLAG GMBH
- Keywords
- Alzheimer' s disease; A beta 42 fibrils; Functionalized benzoxazoles; Binding affinity
- Citation
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.29, no.9, pp.1765 - 1768
- Indexed
- SCIE
SCOPUS
KCI
- Journal Title
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY
- Volume
- 29
- Number
- 9
- Start Page
- 1765
- End Page
- 1768
- URI
- https://scholarworks.bwise.kr/hanyang/handle/2021.sw.hanyang/171893
- DOI
- 10.5012/bkcs.2008.29.9.1765
- ISSN
- 0253-2964
- Abstract
- 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).
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