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噁三唑类NO供体型他汀衍生物的合成及活性评价
引用本文:陈宇瑛,薛雨,艾林,曾其炀. 噁三唑类NO供体型他汀衍生物的合成及活性评价[J]. 中国抗生素杂志, 2020, 45(1): 42-48
作者姓名:陈宇瑛  薛雨  艾林  曾其炀
作者单位:抗生素研究与再评价四川省重点实验室;四川抗菌素工业研究所金华分所;浙江海森药业股份有限公司
基金项目:成都市科技项目(No.2016-XT00-00023-GX)
摘    要:目标 合成系列噁三唑类NO供体型他汀衍生物并进行体外活性评价。方法 选用噁三唑类NO供体分别与阿托伐他汀和辛伐他汀通过酯化进行偶联。结果 设计合成了5个噁三唑类NO供体和5个该类NO供体型他汀衍生物。结论 通过部分目标化合物体外活性测定,表明它们具有良好的NO释放活性。

关 键 词:他汀  噁三唑  合成  NO释放  

Synthesis and activity assay of novel oxatriazole NO donator-type statin derivatives
Chen Yu-ying,Xue Yu,Ai Lin,Zeng Qi-yang. Synthesis and activity assay of novel oxatriazole NO donator-type statin derivatives[J]. Chinese Journal of Antibiotics, 2020, 45(1): 42-48
Authors:Chen Yu-ying  Xue Yu  Ai Lin  Zeng Qi-yang
Affiliation:(Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province,Sichuan Industrial Institute of Antibiotics,Chengdu University,Chengdu 610052;Jinhua Branch of Sichuan Industrial Institute of Antibiotics,Jinhua 321000;Zhejiang Haisen Pharmaceutical Co.,Ltd.,Jinhua 322104)
Abstract:Objective To synthesize a series of novel oxatriazole NO-donating statin derivatives and evaluate their NO release activities in vitro. Methods We used esterification reaction to couple oxatriazole NO-donors and two statins, respectively. Results Five oxatriazole NO-donors and five oxatriazole NO-donating statin derivatives were designed and synthesized. Conclusion The target compounds showed good NO release activity in
Keywords:Statin  Oxatriazole  Synthesis  NO release  
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