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Orally active squalene synthase inhibitors: bis((acyloxy)alkyl) prodrugs of the alpha-phosphonosulfonic acid moiety.

作者信息

Dickson J K, Biller S A, Magnin D R, Petrillo E W, Hillyer J W, Hsieh D C, Lan S J, Rinehart J K, Gregg R E, Harrity T W, Jolibois K G, Kalinowski S S, Kunselman L K, Mookhtiar K A, Ciosek C P

机构信息

Bristol-Myers Sqibb Pharmaceutical Research Institute, Princeton, New Jersey 08543, USA.

出版信息

J Med Chem. 1996 Feb 2;39(3):661-4. doi: 10.1021/jm950735s.

DOI:10.1021/jm950735s
PMID:8576906
Abstract
摘要

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1
Orally active squalene synthase inhibitors: bis((acyloxy)alkyl) prodrugs of the alpha-phosphonosulfonic acid moiety.口服活性角鲨烯合酶抑制剂:α-膦酰基磺酸部分的双((酰氧基)烷基)前药。
J Med Chem. 1996 Feb 2;39(3):661-4. doi: 10.1021/jm950735s.
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Metabolism of alpha-phosphonosulfonate squalene synthase inhibitors. I. Disposition of a farnesylethyl alpha-phosphonosulfonate and ester prodrugs in rats.α-膦酰基磺酸角鲨烯合酶抑制剂的代谢。I. 法呢基乙基α-膦酰基磺酸酯及其酯前药在大鼠体内的处置
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Inhibition of cholesterol synthesis by squalene synthase inhibitors does not induce myotoxicity in vitro.鲨烯合酶抑制剂对胆固醇合成的抑制作用在体外不会诱发肌毒性。
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Synthesis and biological evaluation of novel propylamine derivatives as orally active squalene synthase inhibitors.新型丙胺衍生物作为口服活性角鲨烯合酶抑制剂的合成及生物学评价
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RPR 107393, a potent squalene synthase inhibitor and orally effective cholesterol-lowering agent: comparison with inhibitors of HMG-CoA reductase.RPR 107393,一种有效的角鲨烯合酶抑制剂及口服有效的降胆固醇药物:与HMG-CoA还原酶抑制剂的比较。
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