新型HMG-CoA还原酶抑制剂的合成与生物活性。1. 吡啶和嘧啶取代的3,5-二羟基-6-庚烯酸（-庚酸）内酯
Synthesis and biological activity of new HMG-CoA reductase inhibitors. 1. Lactones of pyridine- and pyrimidine-substituted 3,5-dihydroxy-6-heptenoic (-heptanoic) acids.
作者信息
Beck G, Kesseler K, Baader E, Bartmann W, Bergmann A, Granzer E, Jendralla H, von Kerekjarto B, Krause R, Paulus E
机构信息
Hoechst AG, Frankfurt/M, West Germany.
出版信息
J Med Chem. 1990 Jan;33(1):52-60. doi: 10.1021/jm00163a010.
PMID:2296036
Abstract
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.
摘要
已合成了吡啶和嘧啶取代的3,5 - 二羟基 - 6 - 庚烯酸（- 庚酸）2 - 4的内酯。对构效关系的广泛探索导致了几种化合物在体外和体内对HMG - CoA还原酶的抑制活性超过了美伐他汀（1b）。针对2i（HR 780）的首次临床试验正在筹备中。
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