Literature DB >> 21458990

2-Arylimidazo[2,1-b]benzothiazoles: a new family of amyloid binding agents with potential for PET and SPECT imaging of Alzheimer's brain.

David Alagille1, Herve DaCosta, Ronald M Baldwin, Gilles D Tamagnan.   

Abstract

We designed and synthesized a small series of 2-aryl-imidazo[2,1-b]benzothiazole, representing a combination of motifs from the two most potent amyloid imaging agents, PIB and IMPY. The binding affinity of the new compounds ranged from 6 to 133 nM. Among the best compounds, 3b (K(i)=6 nM) can be labeled with (11)CH(3) for PET imaging whereas 3j (K(i)=10.9 nM) can be labeled with (123)I for SPECT imaging.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21458990     DOI: 10.1016/j.bmcl.2011.03.052

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

1.  On water catalyst-free synthesis of benzo[d]imidazo[2,1-b] thiazoles and novel N-alkylated 2-aminobenzo[d]oxazoles under microwave irradiation.

Authors:  Narasimharao Mukku; Barnali Maiti
Journal:  RSC Adv       Date:  2020-01-03       Impact factor: 4.036

2.  Cell-based HTS identifies a chemical chaperone for preventing ER protein aggregation and proteotoxicity.

Authors:  Keisuke Kitakaze; Shusuke Taniuchi; Eri Kawano; Yoshimasa Hamada; Masato Miyake; Miho Oyadomari; Hirotatsu Kojima; Hidetaka Kosako; Tomoko Kuribara; Suguru Yoshida; Takamitsu Hosoya; Seiichi Oyadomari
Journal:  Elife       Date:  2019-12-17       Impact factor: 8.140

3.  Atomistic investigation of an Iowa Amyloid-β trimer in aqueous solution.

Authors:  Son Tung Ngo; Huong Thi Thu Phung; Khanh B Vu; Van V Vu
Journal:  RSC Adv       Date:  2018-12-13       Impact factor: 3.361

4.  Amyloid-β probes: Review of structure-activity and brain-kinetics relationships.

Authors:  Todd J Eckroat; Abdelrahman S Mayhoub; Sylvie Garneau-Tsodikova
Journal:  Beilstein J Org Chem       Date:  2013-05-28       Impact factor: 2.883

5.  Design, Synthesis, and Structure-Activity Relationships of Thiazole Analogs as Anticholinesterase Agents for Alzheimer's Disease.

Authors:  Begüm Nurpelin Sağlık; Derya Osmaniye; Ulviye Acar Çevik; Serkan Levent; Betül Kaya Çavuşoğlu; Yusuf Özkay; Zafer Asım Kaplancıklı
Journal:  Molecules       Date:  2020-09-20       Impact factor: 4.411

  5 in total

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