Synthesis and evaluation of nimesulide isomeric methoxy/iodo analogs for COX-2 imaging
Project/Area Number |
26861015
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Research Category |
Grant-in-Aid for Young Scientists (B)
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Allocation Type | Multi-year Fund |
Research Field |
Radiation science
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Research Institution | Tohoku Medical and Pharmaceutical University |
Principal Investigator |
YAMAMOTO Yumi 東北医科薬科大学, 薬学部, 助手 (70613446)
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Project Period (FY) |
2014-04-01 – 2017-03-31
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Project Status |
Completed (Fiscal Year 2016)
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Budget Amount *help |
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2016: ¥780,000 (Direct Cost: ¥600,000、Indirect Cost: ¥180,000)
Fiscal Year 2015: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2014: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
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Keywords | COX-2 / イメージング / 画像化 / ニメスリド / 脳 / 物理化学的性質 / 脂溶性 / P糖タンパク質 |
Outline of Final Research Achievements |
The aim of this study is to find suitable radioligands for PET studies which are targeted COX-2 in brain. Nimesulide derivatives are selected as a ligand expecting brain uptake. We synthesized six isomeric methoxy-/iodo- analogs of nimesulide, and evaluated for potential as radioligands for brain COX-2 imaging. All synthesized compounds were shown suitable parameters for favorable brain penetration, and three compounds were found as potent and selective COX-2 inhibitors. Furthermore, three isomeric methoxy analogs of nimesulide have been 14C-radiolabeled. Future studies will aim to develop radiolabeled forms of this nimesulide analog for further in vivo evaluation.
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Report
(4 results)
Research Products
(19 results)
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[Journal Article] Isomeric iodinated analogs of nimesulide: synthesis, physicochemical characterization, cyclooxygenase-2 inhibitory activity, and transport across Caco-2 cells2016
Author(s)
Y. Yamamoto, J. Arai, T. Hisa, Y. Saito, T. Mukai, T. Ohshima, M. Maeda, F. Yamamoto
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Journal Title
Bioorg. Med. Chem.
Volume: 24
Issue: 16
Pages: 3727-3733
DOI
Related Report
Peer Reviewed
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