37. MEP経路を阻害し植物に白化を誘導する化合物の構造活性相関研究

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We reported that clomazone and ketoclomazone inhibited 1-deoxyxylulose-5-phosphate synthase (DXS) in 2-C-methyl-D-erythritol-4-phosphate (MEP) pathway and induced chlorosis to plants. As MEP pathway is indispensable for the formation of isoprenoids not only in plants but also in several bacteria, inhibitors of MEP pathway in plants can be inhibitors of MEP pathway in bacteria and affect the growth of bacteria. That is, such inhibitors could be useful as medical drugs. For example, the target site of fosmidomycin, an antimaralial drug, is the second step of MEP pathway. In this context we started the chemical modification of keto-clomazone and found that some of the derivatives inhibited DXS from E.coli. They also induced chlorosis to plants and this was recovered by the coapplication of DX with inhibitors, suggesting that the target site of these chemicals should be DXS. The relationships between DXS inhibition and chlorosis will be discussed.
2005-10-13