2017 Fiscal Year Final Research Report
Development of the drug candidates with atropisomeric property
| Project/Area Number |
15K08030
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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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(Kenkyū-buntansha) |
児玉 浩子 帝京大学, 医学部, 講師 (00093386)
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| Research Collaborator |
KANASE Yuki
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| Project Period (FY) |
2015-04-01 – 2018-03-31
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| Keywords | 軸不斉 / カルバマゼピン / 光学活性 / ウレア |
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| Outline of Final Research Achievements |
In the course of the research work on the atropisomeric property of urea moiety in the drugs, the physicochemical properties of 4-substituted carbamazepine derivatives were investigated. It was elucidated that the 4-substitution is not effective in reducing the rotations (E/Z) about the N-C1' axes around the outer carbamoyl moiety. However, the atropisomers were isolated with high stereochemical stability, meaning that the 4-substitution reduced the butterfly motion of the tricyclic ring system efficiently. The Cl/CH3-substituted carbamazepine derivatives showed greater inhibitory effects on hNav1.2 Na channel currents compared with carbamazepine, although no difference in the activity between enantiomers was observed.
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| Free Research Field |
創薬化学
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