Lee, Hyu Ji Lim, Soo Jeong Oh, Seung Jun Moon, Dae Hyuk Kim, Dong Jin Tae, Jinsung Yoo, Kyung Ho 2024-01-20T23:33:53Z 2024-01-20T23:33:53Z 2021-08-31 2008-03-01 0960-894X https://pubs.kist.re.kr/handle/201004/133665 Based on the structural features of Indoprofen and PIB, a series of isoindol-1,3-diones 1a-k and isoindol-1-ones 2a-1 were designed and synthesized. These 23 compounds were evaluated by competitive binding assay against aggregated A beta 42 fibrils using [I-125]TZDM. All the isoindolone derivatives showed very good binding affinities with K-i values in the subnanomolar range (0.42-0.94 nM). Among them, isoindol-1,3-diones 1i and 1k and isoindol-1-ones 2c and 2i exhibited excellent binding affinities (K-i = 0.42-0.44 and 0.46-0.49 nM) than those of Indoprofen (K-i = 0.52 nM) and PIB (K-i = 0.70 nM). These results suggest that isoindolones could be served as a scaffold for potential AD diagnostic probes to monitor A beta fibrils. (c) 2008 Elsevier Ltd. All rights reserved. English PERGAMON-ELSEVIER SCIENCE LTD ALZHEIMERS-DISEASE IMAGING AGENTS RISK MEDICINE PLAQUES PROTEIN ONSET Isoindol-1,3-dione and isoindol-1-one derivatives with high binding affinity to beta-amyloid fibrils Article 10.1016/j.bmcl.2008.01.066 1 BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.18, no.5, pp.1628 - 1631 BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 18 5 1628 1631 scie scopus 000254180200017 2-s2.0-40149109194 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article ALZHEIMERS-DISEASE IMAGING AGENTS RISK MEDICINE PLAQUES PROTEIN ONSET Alzheimer&apos s disease A beta 42 fibrils isoindolones binding affinity