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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Nunoya K, Yokoi T, Itoh K, Itoh S, Kimura K, Kamataki T

Division of Drug Metabolism, Faculty of Pharmaceutical Sciences, Hokkaido University, Sapporo, Japan.

Xenobiotica. 1995 Dec;25(12):1283-91. doi: 10.3109/00498259509061917.

Rat hepatic flavin-containing monooxygenase 1 (FMO1) expressed in yeast catalyzed the S-oxidation of (+)-cis-3,5-dimethyl-2-(3-pyridyl)thiazolidin-4-one hydrochloride (SM-12502) in vitro. 2. S-oxidation was inhibited by 1-(1-naphthyl)-2-thiourea and thiobenzamide, known inhibitors of FMO, but was not enhanced by n-octylamine, a known enhancer of FMO. 3. The rate of S-oxide formation from SM-12502 was about four-fold lower than that from (+/-)-trans-3,5-dimethyl-2-(3-pyridyl)thiazolidin-4-one hydrochloride (SM-9979) and enantioselectivity and diastereoselectivity of the S-oxidation reaction were observed. 4. The ability of the recombinant yeast to produce the S-oxide from SM-12502 was maintained for long periods and exemplifies the recombinant yeast as a bioreactor to produce a large amount of the S-oxide.

在酵母中表达的大鼠肝脏含黄素单加氧酶1（FMO1）在体外催化了（+）-顺式-3,5-二甲基-2-（3-吡啶基）噻唑烷-4-酮盐酸盐（SM-12502）的S-氧化反应。2. S-氧化反应受到1-（1-萘基）-2-硫脲和硫代苯甲酰胺（已知的FMO抑制剂）的抑制，但未受到正辛胺（已知的FMO增强剂）的增强。3. 由SM-12502形成S-氧化物的速率比由（±）-反式-3,5-二甲基-2-（3-吡啶基）噻唑烷-4-酮盐酸盐（SM-9979）形成S-氧化物的速率低约四倍，并且观察到了S-氧化反应的对映选择性和非对映选择性。4. 重组酵母从SM-12502产生S-氧化物的能力可长期维持，这证明重组酵母可作为生物反应器大量生产S-氧化物。

Nunoya K, Yokoi T, Itoh K, Itoh S, Kimura K, Kamataki T

Division of Drug Metabolism, Faculty of Pharmaceutical Sciences, Hokkaido University, Sapporo, Japan.

Xenobiotica. 1995 Dec;25(12):1283-91. doi: 10.3109/00498259509061917.

Rat hepatic flavin-containing monooxygenase 1 (FMO1) expressed in yeast catalyzed the S-oxidation of (+)-cis-3,5-dimethyl-2-(3-pyridyl)thiazolidin-4-one hydrochloride (SM-12502) in vitro. 2. S-oxidation was inhibited by 1-(1-naphthyl)-2-thiourea and thiobenzamide, known inhibitors of FMO, but was not enhanced by n-octylamine, a known enhancer of FMO. 3. The rate of S-oxide formation from SM-12502 was about four-fold lower than that from (+/-)-trans-3,5-dimethyl-2-(3-pyridyl)thiazolidin-4-one hydrochloride (SM-9979) and enantioselectivity and diastereoselectivity of the S-oxidation reaction were observed. 4. The ability of the recombinant yeast to produce the S-oxide from SM-12502 was maintained for long periods and exemplifies the recombinant yeast as a bioreactor to produce a large amount of the S-oxide.

在酵母中表达的大鼠肝脏含黄素单加氧酶1（FMO1）在体外催化了（+）-顺式-3,5-二甲基-2-（3-吡啶基）噻唑烷-4-酮盐酸盐（SM-12502）的S-氧化反应。2. S-氧化反应受到1-（1-萘基）-2-硫脲和硫代苯甲酰胺（已知的FMO抑制剂）的抑制，但未受到正辛胺（已知的FMO增强剂）的增强。3. 由SM-12502形成S-氧化物的速率比由（±）-反式-3,5-二甲基-2-（3-吡啶基）噻唑烷-4-酮盐酸盐（SM-9979）形成S-氧化物的速率低约四倍，并且观察到了S-氧化反应的对映选择性和非对映选择性。4. 重组酵母从SM-12502产生S-氧化物的能力可长期维持，这证明重组酵母可作为生物反应器大量生产S-氧化物。