| Project/Area Number |
23790019
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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 |
Chemical pharmacy
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| Research Institution | Kitasato University |
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Principal Investigator |
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| Research Collaborator |
TOMODA Hiroshi 北里大学, 薬学部, 教授 (70164043)
KOYAMA Nobuhiro 北里大学, 薬学部, 助教 (60439156)
SATO Noriko 北里大学, 薬学部, 助教
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| Project Period (FY) |
2011 – 2012
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| Project Status |
Completed (Fiscal Year 2012)
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| Budget Amount *help |
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2012: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2011: ¥2,990,000 (Direct Cost: ¥2,300,000、Indirect Cost: ¥690,000)
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| Keywords | 抗結核薬 / ペプチド / 天然物 / 固相合成 / カルピナクタム / 抗結核剤 |
|---|
| Research Abstract |
Synthesis of calpinactam, a fungal antimycobacterial metabolite, utilizing solid-phase peptide synthesishas been established.To explore the structure-activity relationships(SAR), its derivatives with different amino acids were also synthesized on the basis of the same synthetic strategy.The result of SAR revealed that the side chains, stereochemistry, and entire peptide chain length are essential for antimicobacterial activity. In this study, calpinactam derivative where D-Glu is replaced with D-Ala retained moderate antimycobacterial activity. Furthermore, calpinactam derivative bearing biotin tag was synthesized to elucidate the molecular target
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