2011 Fiscal Year Final Research Report
Elucidation of axial chirality and its application to medicinal chemistry
| Project/Area Number |
21590124
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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 |
Drug development chemistry
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| Research Institution | Teikyo University |
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Principal Investigator |
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| Co-Investigator(Renkei-kenkyūsha) |
TABATA Hidetsugu 帝京大学, 薬学部, 助手 (80445634)
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| Project Period (FY) |
2009 – 2011
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| Keywords | 軸不斉 / キラリティー / γ-セクレターゼ阻害薬 / ACAT阻害薬 / バソプレッシン受容体拮抗薬 / ジベンゾジアゼピノン / ベンゾラクタム |
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| Research Abstract |
The active conformation of biologically active compounds(e. g.,(1) a γ secretase inhibitor, (2) new vasopressin V_1, V_2 receptor antagonists, and (3) new ACAT inhibitors) was elucidated, and the axial chirality originated from an aryl-amide moiety of the molecules was shown to play important role on exerting the activity.
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[Journal Article] Active conformation of seven-membered-ring benzolactams as new ACAT inhibitors : latent chirality at N5 in the 1, 5-benzodiazepin-2-one nucleus2012
Author(s)
Tabata, Hidetsugu ; Wada, Naoya ; Takada, Yuko ; Nakagomi, Jun ; Miike, Tomohiro ; Shirahase, Hiroaki ; Oshitari, Tetsuta ; Takahashi, Hideyo ; Natsugari, Hideaki
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Journal Title
Chemistr-A European Journal
Volume: 18
Pages: 1572-1576
Peer Reviewed
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