首页> 外国专利> AMINO-SUBSTITUTED RUTAECARPIN ANALOG AND SYNTHESIS METHOD AND USE THEREOF IN PREPARATION OF ANTI-OBESITY DRUG

AMINO-SUBSTITUTED RUTAECARPIN ANALOG AND SYNTHESIS METHOD AND USE THEREOF IN PREPARATION OF ANTI-OBESITY DRUG

机译:氨基取代的芸苔素类似物及其合成方法及其在制备抗肥胖药中的应用

摘要

The present invention relates to the fields of pharmaceutical chemistry and pharmaceutical therapeutics. Provided are an amino-substituted rutaecarpin analog and a synthesis method and use thereof in the preparation of an anti-obesity drug. An experiment confirms that the amino-substituted rutaecarpin analog of the present invention can dramatically reduce the lipopexia of 3T3-L1 fat cells, and can reduce the high levulose-induced lipopexia of FAO rat liver cells. A cellular level experiment indicates that the compound can reduce lipopexia, relieve obesity and alleviate fatty liver. The amino-substituted rutaecarpin analog has a chemical formula (I), wherein R0=-NH(CH2)nR2, n=1, 2, 3, 4 or 5, and R2=-N(CH3)2, -N(CH2CH3)2, cyclopentylamino or cyclohexylamino; or R0= morpholinyl, piperazinyl or methylpiperazinyl.
机译:本发明涉及药物化学和药物治疗领域。提供了一种氨基取代的芸苔果胶类似物及其合成方法和在制备抗肥胖药中的用途。实验证实,本发明的氨基取代的芸苔果苷类似物可以显着降低3T3-L1脂肪细胞的脂蛋白血症,并且可以降低高乙酰基葡萄糖诱导的FAO大鼠肝细胞的脂蛋白血症。细胞水平的实验表明该化合物可以减少脂肪过多,减轻肥胖和减轻脂肪肝。氨基取代的芸苔果苷类似物具有化学式(I),其中R 0 =-NH(CH 2 n R 2 ,n = 1、2、3、4或5和R 2 =-N(CH 3 2 ,-N(CH 2 CH 3 2 ,环戊基氨基或环己基氨基;或R 0 =吗啉基,哌嗪基或甲基哌嗪基。

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