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某些3-羟基-5-氨基戊酸衍生物的合成

Synthesis of some 3-hydroxy-5-aminopentanoic acid derivatives.

作者信息

Carganico G, Cangiano G, Cozzi P, Lovisolo P P

出版信息

Farmaco Sci. 1987 Apr;42(4):277-84. doi: 10.1002/chin.198744324.

DOI:10.1002/chin.198744324
PMID:3595839
Abstract

The 5-amino analogues of mevalonic acid and mevalonolactone, 5-amino-3-hydroxy-3-methylpentanoic acid (VII a) and 4-hydroxy-4-methyl-2-piperidone (III a), and some related compounds were synthesized as possible inhibitors of cholesterol biosynthesis. None of them was found effective on the synthesis of cholesterol in rat liver slices and on HMG-CoA reductase activity in vitro, but 4-hydroxy-4-(4-chlorophenyl)-2-piperidone (III b) raised high density lipoproteins (HDL) in normolipaemic rats.

摘要

合成了甲羟戊酸和甲羟戊酸内酯的5-氨基类似物5-氨基-3-羟基-3-甲基戊酸（VII a）和4-羟基-4-甲基-2-哌啶酮（III a）以及一些相关化合物，作为胆固醇生物合成的潜在抑制剂。未发现它们对大鼠肝切片中胆固醇的合成以及体外HMG-CoA还原酶活性有作用，但4-羟基-4-（4-氯苯基）-2-哌啶酮（III b）可使血脂正常的大鼠体内高密度脂蛋白（HDL）升高。

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