RESUMEN
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-bifluorophenyl)-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, compoundwas found to have the best activity, resulting in 80.1% inhibition of ASBT at 10 μmol/L.
RESUMEN
Objective To investigate the relationship between the content of iodide in water and children goiter in the high iodide areas. Methods Pupils aged 8-10 years from 17 primary schools in 10 towns of Huimin county, Yangxin county, Wudi county, Bincheng county were chosen. Based on the contents of water iodide,the pupils were divided into groups, the prevalence of goiter and the content of urinary iodide were determined. Results The prevalence of goiter in the children aged 8-10 was 18.8%,the prevalence showed an increasing tendency. In a certain range, increase of content of iodide in water did not caused an increased prevalence of goiter. There was no association was found between the content of iodide in water and the prevalence of goiter. Conclusion According to the results of the present paper, despite the contents of iodide in drinking water meets the standard of high iodide area, there is still no dose-effect relationship between the prevalence of goiter in the children aged 8-10 years and the content of iodide in water, whereas as the high iodide exposure time prolong, the prevalence of goiter demonstrates an increase tendency.