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Article Navigation >  Journal of Pharmaceutical Practice and Service  > 2015  >  33(6): 525-528,535

TIAN Lin, GUO Haixia, ZHANG Jie, JIAO Yuqiang, WU Qiuye, ZHANG Chuan. Synthesis and anti-myocardial ischemia activities of novel Danshensu derivatives[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(6): 525-528,535. doi: 10.3969/j.issn.1006-0111.2015.06.012
Citation: TIAN Lin, GUO Haixia, ZHANG Jie, JIAO Yuqiang, WU Qiuye, ZHANG Chuan. Synthesis and anti-myocardial ischemia activities of novel Danshensu derivatives[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(6): 525-528,535. doi: 10.3969/j.issn.1006-0111.2015.06.012
shu

Synthesis and anti-myocardial ischemia activities of novel Danshensu derivatives

doi: 10.3969/j.issn.1006-0111.2015.06.012
  • 1.

    niversity of Traditional Chinese Medicine, Fuzhou 350122, China;Department of Science for Identifying Chinese Materia Medica, Second Military Medical University, Shanghai 200433, China

  • 2.

    No.266 Hospital of PLA, Chengde 067000, China

  • 3.

    Second Out-patient Department, National Defence University, Beijing 100039, China

  • 4.

    niversity of Traditional Chinese Medicine, Fuzhou 350122, China;Second Military Medical University, Shanghai 200433, China

  • 5.

    Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China

  • Received Date: 2015-01-23
  • Rev Recd Date: 2015-04-02
  • Objective To design and synthesize novel Danshensu derivatives in order to improve their stability and cardio-protective effect against myocardial ischemia. Methods Novel Danshensu derivatives were synthesized chiefly via esterification,methoxy phenol hydroxyl protection,nitration and amine solution reaction. All the target compounds were evaluated their biological effects on anti-myocardial ischemia with H9c2 cells in vitro. Results 15 compounds were synthesized and further confirmed by 1H NMR and MS. Pharmacological studies showed that few synthetic derivatives at 5 μmol/L performed a higher biological effect than Danshensu. Conclusion Most derivatives didn't show the best activity at the chosen concentration gradient that a further pharmacological trial need to be done.
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    [15] 王定远. 新型丹参素衍生物的合成及初步活性研究[D].广州:广州大学,2011.
    [16] Dong CN,WangY,Zhu YZ.Asymmetric synthesis and biological evaluation of Danshensu derivatives as anti-myocardial ischemia drug candidates[J].Bioorg Med Chem,2009,17:3499-3507.
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Synthesis and anti-myocardial ischemia activities of novel Danshensu derivatives

doi: 10.3969/j.issn.1006-0111.2015.06.012
  • 1. niversity of Traditional Chinese Medicine, Fuzhou 350122, China;Department of Science for Identifying Chinese Materia Medica, Second Military Medical University, Shanghai 200433, China
  • 2. No.266 Hospital of PLA, Chengde 067000, China
  • 3. Second Out-patient Department, National Defence University, Beijing 100039, China
  • 4. niversity of Traditional Chinese Medicine, Fuzhou 350122, China;Second Military Medical University, Shanghai 200433, China
  • 5. Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
  • Received Date: 2015-01-23
  • Rev Recd Date: 2015-04-02

Abstract: Objective To design and synthesize novel Danshensu derivatives in order to improve their stability and cardio-protective effect against myocardial ischemia. Methods Novel Danshensu derivatives were synthesized chiefly via esterification,methoxy phenol hydroxyl protection,nitration and amine solution reaction. All the target compounds were evaluated their biological effects on anti-myocardial ischemia with H9c2 cells in vitro. Results 15 compounds were synthesized and further confirmed by 1H NMR and MS. Pharmacological studies showed that few synthetic derivatives at 5 μmol/L performed a higher biological effect than Danshensu. Conclusion Most derivatives didn't show the best activity at the chosen concentration gradient that a further pharmacological trial need to be done.

TIAN Lin, GUO Haixia, ZHANG Jie, JIAO Yuqiang, WU Qiuye, ZHANG Chuan. Synthesis and anti-myocardial ischemia activities of novel Danshensu derivatives[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(6): 525-528,535. doi: 10.3969/j.issn.1006-0111.2015.06.012
Citation: TIAN Lin, GUO Haixia, ZHANG Jie, JIAO Yuqiang, WU Qiuye, ZHANG Chuan. Synthesis and anti-myocardial ischemia activities of novel Danshensu derivatives[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(6): 525-528,535. doi: 10.3969/j.issn.1006-0111.2015.06.012
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