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

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

doi:10.1016/j.bmcl.2008.05.019

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

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

Department of Pharmacy

Research output: Contribution to journal › Article › peer-review

15 Citations (Scopus)

Abstract

In this study a novel series of isoindol-1-one and isoindol-1,3-dione derivatives for β-amyloid-specific binding agents is described. Twelve compounds were synthesized and evaluated via a competitive binding assay with [¹²⁵I]TZDM against β-amyloid 1-42 (Aβ42) aggregates. Two new [¹⁸F]-labeled isoindole derivatives were synthesized and evaluated as potential β-amyloid imaging probes based on the in vivo pharmacokinetic profiles. The preliminary results suggest that these [¹⁸F]18b and [¹⁸F]18c are promising positron emission tomography (PET) imaging probes for studying accumulation of Aβ fibrils in the brains of Alzheimer's disease (AD) patients.

Original language	English
Pages (from-to)	5701-5704
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	20
DOIs	https://doi.org/10.1016/j.bmcl.2008.05.019
Publication status	Published - 2008 Oct 15

Bibliographical note

Funding Information:
We are grateful to the Ministry of Science and Technology (MOST) and Ministry of Commerce, Industry and Energy (MCIE) of Korea for financial support.

All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2008.05.019

Cite this

@article{2f4d31aa99354e83bb40406d8a203fe9,

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

abstract = "In this study a novel series of isoindol-1-one and isoindol-1,3-dione derivatives for β-amyloid-specific binding agents is described. Twelve compounds were synthesized and evaluated via a competitive binding assay with [125I]TZDM against β-amyloid 1-42 (Aβ42) aggregates. Two new [18F]-labeled isoindole derivatives were synthesized and evaluated as potential β-amyloid imaging probes based on the in vivo pharmacokinetic profiles. The preliminary results suggest that these [18F]18b and [18F]18c are promising positron emission tomography (PET) imaging probes for studying accumulation of Aβ fibrils in the brains of Alzheimer's disease (AD) patients.",

author = "Lee, {Ji Hoon} and Byeon, {Seong Rim} and Kim, {Young Soo} and Lim, {Soo Jeong} and Oh, {Seung Jun} and Moon, {Dae Hyuk} and Yoo, {Kyung Ho} and Chung, {Bong Young} and Kim, {Dong Jin}",

note = "Funding Information: We are grateful to the Ministry of Science and Technology (MOST) and Ministry of Commerce, Industry and Energy (MCIE) of Korea for financial support.",

year = "2008",

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doi = "10.1016/j.bmcl.2008.05.019",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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T1 - [18F]-labeled isoindol-1-one and isoindol-1,3-dione derivatives as potential PET imaging agents for detection of β-amyloid fibrils

AU - Lee, Ji Hoon

AU - Byeon, Seong Rim

AU - Kim, Young Soo

AU - Lim, Soo Jeong

AU - Oh, Seung Jun

AU - Moon, Dae Hyuk

AU - Yoo, Kyung Ho

AU - Chung, Bong Young

AU - Kim, Dong Jin

N1 - Funding Information: We are grateful to the Ministry of Science and Technology (MOST) and Ministry of Commerce, Industry and Energy (MCIE) of Korea for financial support.

PY - 2008/10/15

Y1 - 2008/10/15

N2 - In this study a novel series of isoindol-1-one and isoindol-1,3-dione derivatives for β-amyloid-specific binding agents is described. Twelve compounds were synthesized and evaluated via a competitive binding assay with [125I]TZDM against β-amyloid 1-42 (Aβ42) aggregates. Two new [18F]-labeled isoindole derivatives were synthesized and evaluated as potential β-amyloid imaging probes based on the in vivo pharmacokinetic profiles. The preliminary results suggest that these [18F]18b and [18F]18c are promising positron emission tomography (PET) imaging probes for studying accumulation of Aβ fibrils in the brains of Alzheimer's disease (AD) patients.

AB - In this study a novel series of isoindol-1-one and isoindol-1,3-dione derivatives for β-amyloid-specific binding agents is described. Twelve compounds were synthesized and evaluated via a competitive binding assay with [125I]TZDM against β-amyloid 1-42 (Aβ42) aggregates. Two new [18F]-labeled isoindole derivatives were synthesized and evaluated as potential β-amyloid imaging probes based on the in vivo pharmacokinetic profiles. The preliminary results suggest that these [18F]18b and [18F]18c are promising positron emission tomography (PET) imaging probes for studying accumulation of Aβ fibrils in the brains of Alzheimer's disease (AD) patients.

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