2014 Fiscal Year Final Research Report
Stereochemistry based on the axial chirality and development of novel bioactive compounds
| Project/Area Number |
25860091
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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 | Teikyo University |
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Principal Investigator |
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| Project Period (FY) |
2013-04-01 – 2015-03-31
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| Keywords | 軸不斉 / アミド構造 / 連動性 |
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| Outline of Final Research Achievements |
The stereochemistry of N-benzoyl-1,5-benzothiazepine and its S-oxide derivatives as vasopressin receptor ligands was examined in detail by freezing the conformation with a methyl group at the C6 or C9 of 1,5-benzothiazepine. It was revealed that the active forms recognized by the receptors are (cis, aS) for 1,5-benzothiazepine and (cis, 1S, aS) (syn) for its S-oxide. The C9-methyl derivative of 1,5-benzothiazepine S-oxide was designed and synthesized, achieving the putative active syn-stereochemistry.
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| Free Research Field |
医歯薬学
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