65329-03-5Relevant articles and documents
Tanshinol and H2 S/NO Donor binding, preparation method thereof and application in pharmacy (by machine translation)
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Paragraph 0080-0082, (2020/08/18)
The invention belongs to the field of chemical pharmacy, and relates to active ingredient tanshinol and H in Chinese herbal medicine Salvia miltiorrhiza. 2 S/NO Donors and its preparation method and use in pharmacy, especially in the preparation of medicines for preventing and treating cardiovascular and cerebrovascular diseases and inflammation related diseases. To the invention, through in-vitro oxidative stress injury and inflammation model experiments, the results show that H is obviously inhibited. 2 O2 In vivo activity experiment results show that the conjugate is capable of remarkably inhibiting the release of inflammatory cytokines induced by LPS (LPS), reducing inflammation-induced mouse peritoneal macrophages, obviously inhibiting the release of inflammatory cytokines induced by LPS, and showing the result that the compound can be used for preparing drugs for preventing and treating cardiovascular and cerebrovascular diseases and inflammatory diseases. (by machine translation)
Improved process for pilot-scale synthesis of danshensu ((±)-DSS) and its enantiomer derivatives
Bai, Yajun,Zhang, Qunzheng,Jia, Pu,Yang, Lingjian,Sun, Yuhong,Nan, Yefei,Wang, Shixiang,Meng, Xue,Wu, Yizhen,Qin, Fanggang,Sun, Zhe,Gao, Xiaokang,Liu, Pei,Luo, Kai,Zhang, Yajun,Zhao, Xinfeng,Xiao, Chaoni,Liao, Sha,Liu, Jianli,Wang, Cuiling,Fang, Jiacheng,Wang, Xiaoxiao,Wang, Jing,Gao, Rong,An, Xuexia,Zhang, Xunli,Zheng, Xiaohui
, p. 1667 - 1673 (2015/02/18)
A pilot-scale process has been developed for green and scalable synthesis of (±)-β-(3,4-dihydroxyphenyl) lactic acid ((±)-DSS) and their two important derivatives, namely, (±)-IDHP [(±)-isopropyl 2-hydroxy-3-(3,4-dihydroxyphenyl)propanoate] and (±)-DBZ [(±)-bornyl 2-hydroxy-3-(3,4-dihydroxyphenyl)propanoate]. Subsequent hydrogenation has been carried out by employing Raney Ni as catalyst. The improved process results in higher yields of 47.5% for (±)-DBZ and 49.2% for (±)-IDHP compared to the initial process with a yield of 12% for (±)-DBZ and 18% for (±)-IDHP in our original medicinal chemistry route. Furthermore, kilograms of optical DBZ [(-)-S-DBZ and (+)-R-DBZ, >99% ee] and IDHP [(-)-S-IDHP and (+)-R-IDHP, >99% ee] have been produced by chiral high-performance liquid chromatography in good yield (>84%).
The synthesis and biological evaluation of novel Danshensu-cysteine analog conjugates as cardiovascular-protective agents
Jia, Yaoling,Zhou, Pengfei,Wang, Yang,Dong, Xiaoyi,Liu, Xinhua,Pan, Lilong,Xin, Hong,Zhu, Yi Zhun
, p. 176 - 187,12 (2020/07/31)
A series of novel amide and thioester conjugates between Danshensu and cysteine derivatives have been designed and synthesized based on the strategy of "medicinal chemical hybridization". Pharmacological evaluation indicated that the amide conjugates 3a/4a/17a and thioester conjugates 6a-d exhibited obvious protective effects on H2O2-induced human umbilical vein endothelial cells (HUVECs). Pretreated with these conjugates could increase glutathione (GSH) activity and decrease malondialdehyde (MDA) level. Further study on mechanism of compound 4a revealed that it was related to its mitochondrial-protective effect and regulation of apoptosis-related proteins expression (Bax, p53, PARP, caspase-3, caspase-9 and Bcl-2). These results indicate that these Danshensu-cysteine analog conjugates possess significant cardiovascular-protective effects and merit further investigation.
