2012 Fiscal Year Final Research Report
Development of novel antibacterial leads based on natural products
| Project/Area Number |
22689004
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| Research Category |
Grant-in-Aid for Young Scientists (A)
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| Allocation Type | Single-year Grants |
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| Research Field |
Drug development chemistry
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| Research Institution | Hokkaido University |
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Principal Investigator |
ICHIKAWA Satoshi 北海道大学, 大学院・薬学研究院, 准教授 (60333621)
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| Project Period (FY) |
2010 – 2012
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| Keywords | 天然物 / 有機合成 / 創薬化学 / 薬剤耐性菌 |
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| Research Abstract |
The caprazamycins (CPZs), muraymycins (MRYs), and mureidomycins (MRDs) which constitute a class of nucleoside natural products, exhibit excellent antimicrobial activity against. This work presents a total synthesis, systematic structure-activity relation-ship (SAR) study, and simplification of CPZs, MRYs, and MRDs. The analogues exhibited good activity against a range of Gram-positive bacterial pathogens, including MRSA and VRE. The oxazolidine analogues were developed through simplification of CPZs, and they exhibited antibacterial activity with a similar potency to the CPZs. Our SAR study of the CPZs and MRYs suggests a probable mechanism for inhibition of the MraY.
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