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Synthesis and evaluation of stilbenylbenzoxazole and stilbenylbenzothiazole derivatives for detecting beta-amyloid fibrils
- Authors
- Lee, Ji Hoon; Byeon, Seong Rim; Lim, Soo Jeong; Oh, Seung Jun; Moon, Dae Hyuk; Yoo, Kyung Ho; Chung, Bong Young; Kim, Dong Jin
- Issue Date
- 15-2월-2008
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Alzheimer' s disease; beta-amyloid fibrils; PET imaging
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.18, no.4, pp.1534 - 1537
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 18
- Number
- 4
- Start Page
- 1534
- End Page
- 1537
- ISSN
- 0960-894X
- Abstract
- This paper describes a novel series of stilbenylbenzoxazole ( SBO) and stilbenylbenzothiazole ( SBT) derivatives for beta- amyloid specific binding probes. These 24 compounds were synthesized and evaluated by competitive binding assay against beta- amyloid 1 - 42 ( A beta 42) aggregates using [I-125] TZDM. All the derivatives displayed higher binding affinities with K-i value in the subnanomolar range ( 0.10 - 0.74 nM) than Pittsburgh Compound- B ( PIB) ( 0.77 nM). Among these derivatives, SBT- 2, 5-. uoroethoxy- 2-{ 4-[ 2-( 4- methylaminophenyl) vinyl] phenyl} benzothiazole, showed lowest K-i value ( 0.10 nM). In conclusion, the preliminary results suggest that these compounds are implying a possibility as a probe for detection of A beta fibrils in Alzheimer's disease (AD) patients. (C) 2007 Elsevier Ltd. All rights reserved.
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