含取代异噁唑的白桦脂醇衍生物的设计、合成及其蛋白酪氨酸磷酸酯酶1B抑制活性
收稿日期: 2016-11-14
修回日期: 2016-12-07
网络出版日期: 2016-12-12
基金资助
江苏省自然科学基金青年（No. BK20140425）、南通大学引进人才科研启动费（No. 03080694）资助项目.
Design, Synthesis of Betulin Derivatives Containing 5-Phenyl-3-isoxazole and Their Inhibitory Activities against Protein Tyrosine Phosphatase 1B
Received date: 2016-11-14
Revised date: 2016-12-07
Online published: 2016-12-12
Supported by
Project supported by the Science Fund for Young Scholar of Jiangsu Province (No. BK20140425) and the Initiating Fund for Introduced Talents of Nantong University (No. 03080694).
何海兵 , 戴红 , 葛英花 , 施磊 , 邹政 , 叶飞 , 金甲 , 石玉军 . 含取代异噁唑的白桦脂醇衍生物的设计、合成及其蛋白酪氨酸磷酸酯酶1B抑制活性[J]. 有机化学, 2016 , 36(12) : 2888 -2894 . DOI: 10.6023/cjoc201611016
Protein tyrosine phosphatase-1B (PTP1B) is recognized as a potent target for the therapy of diabetes. By introducing substituted 5-phenyl-3-isoxazole ring to the 3-position of betulin, a series of novel compounds were designed, synthesized and characterized by 1H NMR, 13C NMR and HRMS. The results of bioassays exhibited that most of the titled compounds were active to PTP1B. Among them, compound 15h has an IC50 of 0.98 μmol·L-1 against PTP1B and a 4-fold selectivity over T cell protein tyrosine phosphatase (TCPTP).
Key words： PTP1B Inhibitor; TCPTP; Betulin; Synthesis
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