2016 Fiscal Year Final Research Report
Discovery of muscarinic acetylcholine receptor partial agonists
| Project/Area Number |
15K18903
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Drug development chemistry
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| Research Institution | Kansai University |
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Principal Investigator |
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| Research Collaborator |
NAKAMURA Arisa
NAMBARA Takuya
MURAKAMI Masato
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| Project Period (FY) |
2015-04-01 – 2017-03-31
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| Keywords | ムスカリン受容体作動薬 / 部分作動薬 / 創薬化学 / 光学活性体 / 構造活性相関 |
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| Outline of Final Research Achievements |
Muscarinic acetylcholine receptors (M1-M5) are potent drug targets for the treatment of various central nerve system diseases. Among the subtypes, activation of M1 receptor leads to improvement of cognitive impairment. Although many medicinal chemists have challenged to discover selective M1 agonists, most of the compounds did not show enough high subtype-selectivity to dissociate the side effects.
In this study, we synthesized benzimidazolone derivatives and identified subtype selective M1 receptor partial agonists based on the structure-activity relationship information. The identified compounds are potent for the treatment central nerve system diseases.
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| Free Research Field |
創薬化学
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