Synthesis and biological evaluations of quinoline-based HMG-CoA reductase inhibitors

…, H Iwasaki, Y Fujikawa, M Kitahara, M Sakashita…

文献索引：Suzuki; Iwasaki; Fujikawa; Kitahara; Sakashita; Sakoda Bioorganic and Medicinal Chemistry, 2001 ,  vol. 9,  # 10  p. 2727 - 2743

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被引用次数: 94

摘要

A series of quinoline-based 3, 5-dihydroxyheptenoic acid derivatives were synthesized from quinolinecarboxylic acid esters by homologation, aldol condensation with ethyl acetoacetate dianion, and reduction of 3-hydroxyketone to evaluate their ability to inhibit the enzyme HMG- CoA reductase in vitro. In agreement with previous literature, a strict structural requirement exists on the external ring, and 4-fluorophenyl is the most active in this system. For the ...