2015 Fiscal Year Final Research Report
Development of new modification methods of peptide terminal using carbophilic Lewis acid and a new peptide isostere
| Project/Area Number |
25860005
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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 | Osaka University |
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Principal Investigator |
AIKAWA Haruo 大阪大学, 産業科学研究所, 助教 (70547322)
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| Project Period (FY) |
2013-04-01 – 2016-03-31
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| Keywords | ペプチド / アルキル化 / オキサザボロリジン / イソスター / カチオン性触媒 / ゲル |
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| Outline of Final Research Achievements |
In the studies of development of new peptide-modification reactions, benzylation of benzoic amide was successfully proceeded in the presence of cationic gold catalyst.
Oxazaborolidine was successfully introduced to FC131, cyclic pentapeptide which can bind to CXCR4, and ESI-MS showed cyclic product, mono-hydrated product, and dihydrated product peaks. This isostere did not show anti-HIV-1 activity and cytotoxicity at 10 microM.
Fmoc-amino acid revealed to be very effective gelator of non-polar organic solvent such as chloroform and hexane.
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| Free Research Field |
有機合成化学
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