2011 Fiscal Year Final Research Report
Development of Novel Methodology for the Synthesis of 2, 3-Benzodiazepines and Application for Neuro-therapeutic Agents
| Project/Area Number |
21590006
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Chemical pharmacy
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| Research Institution | University of Toyama |
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Principal Investigator |
MATSUYA Yuji 富山大学, 大学院・医学薬学研究部(薬学), 教授 (50255858)
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| Co-Investigator(Renkei-kenkyūsha) |
TOHDA Chihiro 富山大学, 和漢医薬学総合研究所, 准教授 (10272931)
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| Project Period (FY) |
2009 – 2011
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| Keywords | ベンゾジアゼピン / ジアザベンゾトロポン / AMPAレセプター / 神経性疾患 / 電子環状反応 / アポトーシス誘導 / 抗癌活性 |
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| Research Abstract |
Synthetic and medicinal studies of 2, 3-benzodiazepine derivatives were performed for the purpose of exploring novel drug seeds of neuronal disorders. We could establish new method of constructing 2, 3-benzodiazepine nucleus based on our original tandem electrocyclic reactions using benzocyclobutenes and diazomethylene anion as starting materials, and succeed in constructing a novel diazabenzotropone compounds library. Although these compounds were found not to exhibit neuronal protecting activity, some of them showed notable apoptosis-inducing activity against some lymphoma cells. Thus, we found that novel diazabenzotropone derivatives, synthesized utilizing our original reactions, could be a new candidate of novel anticancer agents.
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[Journal Article] Novel 3, 4-Diazabenzotropone Compounds(2, 3-Benzodiazepin-5-ones): Synthesis, Unique Reactivity, and Biological Evaluation2009
Author(s)
Matsuya, Y.; Katayanagi, H.; Ohdaira, T.; Wei, Z.-L.; Kondo, T.; Nemoto, H.
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Journal Title
Org. Lett
Volume: 11
Pages: 1361-1364
Peer Reviewed
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