绿卡色林衍生物的合成、体外代谢及体内活性研究

发布时间：2018-03-30 18:15

本文选题：绿卡色林　切入点：前药　出处：《高等学校化学学报》2017年10期

【摘要】：将选择性5-HT2C受体激动剂类减肥药绿卡色林分子中的仲胺转化成氨基甲酸酯类前药,设计合成了13个氨基甲酸酯类化合物.新化合物的结构经核磁共振波谱、红外光谱及高分辨质谱确证.通过体外代谢稳定性实验,筛选出半衰期长且可通过代谢持续产生绿卡色林的新化合物6b.对化合物6b的大鼠减肥药理实验结果表明,在日剂量相同的条件下,化合物6b给药1次/d比绿卡色林给药2次/d的减肥效果略好.
[Abstract]:Thirteen carbamate compounds were designed and synthesized by converting secondary amines from the selective 5-HT2C receptor agonists into carbamate prodrugs.The structure of the new compound was confirmed by NMR, IR and high resolution mass spectrometry.By in vitro metabolic stability experiment, a new compound with long half-life and sustained production of green Casserin was screened out.Under the same daily dosage, compound 6b was given once a day, and the effect was slightly better than that of green carbazepine for two times a day, the results showed that the pharmacological effect of compound 6b on rat diet was better than that of green carbazepine for two times a day at the same daily dose.
【作者单位】：中国药科大学药物化学系;中国药科大学药理系;南京医工医药技术有限公司;
【基金】：江苏省产学研前瞻性联合研究项目(批准号:BY2015072-02)资助~~
【分类号】：R914;TQ460.1

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