[F-18]-labeled isoindol-1-one and isoindol-1,3-dione derivatives as potential PET imaging agents for detection of beta-amyloid fibrils

Lee, Ji Hoon; Byeon, Seong Rim; Kim, YoungSoo; Lim, Soo Jeong; Oh, Seung Jun; Moon, Dae Hyuk; Yoo, Kyung Ho; Chung, Bong Young; Kim, Dong Jin

doi:10.1016/j.bmcl.2008.05.019

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[F-18]-labeled isoindol-1-one and isoindol-1,3-dione derivatives as potential PET imaging agents for detection of beta-amyloid fibrils

Lee, Ji Hoon;
Byeon, Seong Rim;
Kim, YoungSoo;
Lim, Soo Jeong;
Oh, Seung Jun;
외 4명

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19

초록

In this study a novel series of isoindol-1-one and isoindol-1,3-dione derivatives for beta-amyloid-specific binding agents is described. Twelve compounds were synthesized and evaluated via a competitive binding assay with [I-125]TZDM against beta-amyloid 1-42 (A beta 42) aggregates. Two new [F-18]-labeled isoindole derivatives were synthesized and evaluated as potential beta-amyloid imaging probes based on the in vivo pharmacokinetic profiles. The preliminary results suggest that these [F-18]18b and [F-18]18c are promising positron emission tomography (PET) imaging probes for studying accumulation of A beta fibrils in the brains of Alzheimer's disease (AD) patients. (C) 2008 Elsevier Ltd. All rights reserved.

키워드

Alzheimer's disease; [F-18]-labeled; PET; imaging probe; ALZHEIMERS-DISEASE; NEUROFIBRILLARY TANGLES; PLAQUES; MEDICINE; BINDING

제목: [F-18]-labeled isoindol-1-one and isoindol-1,3-dione derivatives as potential PET imaging agents for detection of beta-amyloid fibrils

저자: Lee, Ji Hoon; Byeon, Seong Rim; Kim, YoungSoo; Lim, Soo Jeong; Oh, Seung Jun; Moon, Dae Hyuk; Yoo, Kyung Ho; Chung, Bong Young; Kim, Dong Jin

DOI: 10.1016/j.bmcl.2008.05.019

발행일: 2008-10-15

유형: Article

저널명: Bioorganic & Medicinal Chemistry Letters

권: 18

호: 20

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