1262896-06-9Relevant academic research and scientific papers
MATRINIC ACID/MATRINE DERIVATIVES AND PREPARATION METHODS AND USES THEREOF
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Paragraph 0629, (2013/07/31)
The present invention relates to a N-substituted matrinic acid derivative or matrine derivative, and its preparation method and uses. Specifically, the present invention relates to a compound of Formula (I) or (II) (wherein all the definitions of substituted groups are those mentioned in the specification), or a pharmaceutically acceptable salt, geometric isomer, stereoisomer, solvate, ester or prodrug thereof. The present invention further relates to a method for preparing the compound of the present invention, a pharmaceutical composition containing the compound, and uses thereof in manufacture of a medicament. The compound of the present invention can be used for prophylaxis and/or treatment of a disease or disorder associated with viral infection such as hepatitis B and/orhepatitis C and/or AIDS.
MATRINIC ACID/ MATRINE DERIVATIVES AND PREPARATION METHODS AND USES THEREOF
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, (2013/04/25)
The present invention relates to a N-substituted matrinic acid derivative or matrine derivative, and its preparation method and uses. Specifically, the present invention relates to a compound of Formula (I) or (II) (wherein all the definitions of substituted groups are those mentioned in the specification), or a pharmaceutically acceptable salt, geometric isomer, stereoisomer, solvate, ester or prodrug thereof. The present invention further relates to a method for preparing the compound of the present invention, a pharmaceutical composition containing the compound, and uses thereof in manufacture of a medicament. The compound of the present invention can be used for prophylaxis and/or treatment of a disease or disorder associated with viral infection such as hepatitis B and/orhepatitis C and/orAIDS.
Design and synthesis of oxymatrine analogues overcoming drug resistance in hepatitis B virus through targeting host heat stress cognate 70
Gao, Li-Mei,Han, Yan-Xing,Wang, Yu-Ping,Li, Yu-Huan,Shan, Yong-Qiang,Li, Xin,Peng, Zong-Gen,Bi, Chong-Wen,Zhang, Tian,Du, Na-Na,Jiang, Jian-Dong,Song, Dan-Qing
, p. 869 - 876 (2011/04/18)
Heat-stress cognate 70 (Hsc70is a host protein required for hepatitis B virus (HBVreplication, and oxymatrine (1suppresses Hsc70 expression. Taking Hsc70 as a target against HBV, 22 analogues of 1 defined with substituents at position 1, 13, or 14 were synthesized and evaluated for their activity on Hsc70 mRNA expression. The SAR revealed that (ithe oxygen atom at the 1-position was not essential, (iiincreasing electron density on the ring D reduced the activity, and (iiiintroducing a proper substituent at the 13-and/or 14-position(s), especially electron-withdrawing groups, might enhance the activity. Among the analogues, 6b possessing 13-ethoxyl afforded an increased activity in respect to 1. Importantly, it was active for either wild-type or lamivudine-resistant HBV, as its target is host Hsc70 but not viral enzymes. LD50 of 6b in mice was over 750 mg/kg in oral route. We consider compound 6b promising for further investigation.
