Mechanism of antioxidative activity of fluvastatin-determination of the active position.
Mechanism of antioxidative activity of fluvastatin-determination of the active position.
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氟伐他汀抗氧化活性机制——活性位置的测定。
DOI：
10.1248/cpb.48.235
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发表时间：
2000
影响因子：
1.7
通讯作者：
Y. Miura
中科院分区：
文献类型：
--
作者：
Takashi Nakamura;Hiroyuki Nishi;Y. Kokusenya;Kenichi Hirota;Y. Miura
为了阐明氟伐他汀钠(FLV,(+/-)-钠（3RS, 5RS, 6E)-7-[3-（4-氟苯基）-1-（1-甲基乙基）- 1h -吲哚-2-基]- 3,5 -二羟基-6-庚酸酯）及其衍生物的抗氧化作用机理，研究了FLV相应的甲酯与二过氧草酸二叔丁基的反应，并从反应混合物中分离出相应的酮类衍生物。在此基础上，得出了活性位点为烯丙碳与吲哚环共轭的结论。
In order to clarify the mechanism of action for the antioxidative activity of fluvastatin sodium (FLV, (+/-)-sodium (3RS, 5RS, 6E)-7-[3-(4-fluorophenyl)-1-(1-methylethyl)-1H-indol-2-yl]-3, 5-dihydroxy-6-heptanoate) and its derivatives, reaction of the corresponding methyl ester of FLV with di-tert-butyl diperoxyoxalate was examined, and the corresponding keto derivative was isolated from the reaction mixture. On the basis of this result, it was concluded that the active site is the allylic carbon conjugated with the indole ring.