期刊
ACTA PHARMACEUTICA SINICA B
卷 7, 期 2, 页码 223-229出版社
INST MATERIA MEDICA, CHINESE ACAD MEDICAL SCIENCES
DOI: 10.1016/j.apsb.2016.11.005
关键词
ASBT inhibitors; Bile acids; 1-(2,4-Bifluompheny1)-7-dialkylamino-1,8-naphthyridine-3-carboxa mides; Cholesterol-lowering drug; NC-1
资金
- National Natural Science Foundation of China [81473098, 81473099]
- Hebei Provincial Key Research Project of Medical Science [ZD20140027, 20150588]
The apical sodium dependent bile acid transporter (ASBT) is the main transporter to promote re-absorption of bile acids from the intestinal tract into the enterohepatic circulation. Inhibition of ASBT could increase the excretion of bile acids, thus increasing bile acid synthesis and consequently cholesterol consumption. Therefore, ASBT is an attractive target for developing new cholesterol-lowering drugs. In this report, a series of 1-(2,4-bifluoropheny1)-7-dialkylamino-1,8-naphthyridine-3-carboxamides were designed as inhibitors of ASBT. Most of them demonstrated potency against ASBT transport of bile acids. In particular, compound 4a(1) was found to have the best activity, resulting in 80.1% inhibition of ASBT at 10 mu mol/L. (C) 2017 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.
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