New Strong Fibrates with Piperidine Moiety.
作者:Teruo KOMOTO、Hiroyuki HIROTA、Mari OTSUKA、Jiro KOTAKE、Susumu HASEGAWA、Hidehiko KOYA、Susumu SATO、Takao SAKAMOTO
DOI:10.1248/cpb.48.1978
日期:——
New fibrates containing piperidine, 4-hydroxypiperidine, piperidin-3-ene, and piperazine moieties in the structures were synthesized and evaluated. Among the synthesized compounds, 2-[3-[1-(4-fluorobenzoyl)-piperidin-4yl]phenoxy]-2-methylpropanoic acid (9aA : AHL-157) showed very superior activities in decreasing triglyceride, cholesterol, and blood sugar compared to bezafibrate in mice and rats.
合成并评估了结构中含有哌啶、4-羟基哌啶、哌啶-3-烯和哌嗪分子的新型纤维化合物。在合成的化合物中,2-[3-[1-(4-氟苯甲酰基)-哌啶-4-基]苯氧基]-2-甲基丙酸(9aA : AHL-157)在降低小鼠和大鼠甘油三酯、胆固醇和血糖方面的活性优于贝扎贝特。