SYNTHESIS AND BIOLOGICAL-ACTIVITY OF NEW HMG-COA REDUCTASE INHIBITORS .1. LACTONES OF PYRIDINE-SUBSTITUTED AND PYRIMIDINE-SUBSTITUTED 3,5-DIHYDROXY-6-HEPTENOIC (-HEPTANOIC) ACIDS

被引：67

作者：

BECK, G ^{[1
]}

KESSELER, K ^{[1
]}

BAADER, E ^{[1
]}

BARTMANN, W ^{[1
]}

BERGMANN, A ^{[1
]}

GRANZER, E ^{[1
]}

JENDRALLA, H ^{[1
]}

VONKEREKJARTO, B ^{[1
]}

KRAUSE, R ^{[1
]}

PAULUS, E ^{[1
]}

SCHUBERT, W ^{[1
]}

WESS, G ^{[1
]}

机构：

[1] HOECHST AG,POSTFACH 800320,W-6230 FRANKFURT 80,GERMANY

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1990年 / 33卷 / 01期

关键词：

D O I：

10.1021/jm00163a010

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Lactones of pyridine- and pyrimidine-substituted 3,5-dihydroxy-6-heptenoic (-heptanoic) acids 2-4 have been synthesized. Extensive exploration of structure-activity relationships led to several compounds exceeding the inhibitory activity of mevinolin (1b) on HMG-CoA reductase, both in vitro and in vivo. First clinical trials with 2i (HR 780) are in preparation. © 1990, American Chemical Society. All rights reserved.

引用

页码：52 / 60

页数：9

共 34 条

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