Scaffold Evaluation of Liguzinediol Analogs as Novel Cardiotonic Agents

LIU Zheng; LI Wei; QIN Kai; WEN Kan; ZHU Chenjian; LI Nianguang; BIAN Huimin; WEN Hongmei; CHEN Long

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Scaffold Evaluation of Liguzinediol Analogs as Novel Cardiotonic Agents

LIU Zheng 1 #,LI Wei 1 *,QIN Kai 1,WEN Kan 1,ZHU Chenjian 2,LI Nianguang 1,BIAN Huimin 1,WEN Hongmei 1,CHEN Long 1

1.School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046

2. School of Chemistry and Chemical Engineering, Nanjing University, Nanjing 210093

*Correspondence author

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Funding: This work was financially supported by National Natural Science Foundation of China （No.81072542）, the Major Scientific and Technological Special Project（No.2009ZX09103-081）, the Specialized Research Fund for the Doctoral Program of Higher Education of China （No.20123237110010）

Opened online:25 April 2013

Accepted by: none

Citation: LIU Zheng,LI Wei,QIN Kai.Scaffold Evaluation of Liguzinediol Analogs as Novel Cardiotonic Agents[OL]. [25 April 2013] http://en.paper.edu.cn/en_releasepaper/content/4538513

Liguzinediol (LZDO) could mediate the positive inotropic effects through sarcoplasmic reticulum Ca2+ ATPase-dependent mechanism without the risk of arrhythmia. However, the pharmacophore of LZDO contributed to the activities was not clear. The aim of this work is to explore the relationship between positive inotropic effect and scaffold of LZDO as well as to check whether the pharmacophore of LZDO on anti-heart failure activity was located at the pyrazine ring. A series of LZDO analogs (3a-b, 4a-b, 9-19) were designed and synthesised, and their activities were evaluated on isolated heart contractility by Langendorff perfusion. The results showed that the efficacy of LZDO was reduced when the hydroxyl, carboxyl or ester moieties at the side chain position of LZDO were induced, and the para-dihydroxy in LZDO was necessary for its activity. Thus, the pharmacophore of positive inotropic effect might be located at the whole scaffold of LZDO, but not at the pyrazine ring. The finding may provide important clue of pharmacophore for the development of novel cardiotonic agents.

Keywords:Liguzinediol; Liguzindiol analogs; Synthesis; Positive inotropic effect; Structure-based compound design

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