title: Synthesis and positive inotropic activity evaluation of liguzinediol metabolites.
abstract: 2,5-Dihydroxymethyl-3,6-dimethylpyrazine (liguzinediol) has been recently discovered as a potential agent for treatment of heart failure with low safety risk. In the present study, four main metabolites of liguzinediol were synthesized and their positive inotropic activities were evaluated. Synthetic compounds were identical with the isolated metabolites of liguzinediol. Pharmacological examinations showed that the four major metabolites were not observed positive inotropic activity, and revealed that the positive inotropic activity of liguzinediol was essentially attributed to the parent agent.
authors.affiliation: School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing 210023, Jiangsu, China.
authors.forename: Hao-Hao
authors.initials: HH
authors.lastname: Zhu
authors.affiliation: School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing 210023, Jiangsu, China.
authors.forename: Yu-Qing
authors.initials: YQ
authors.lastname: Chen
authors.affiliation: School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing 210023, Jiangsu, China.
authors.forename: Dong
authors.initials: D
authors.lastname: Cheng
authors.affiliation: School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing 210023, Jiangsu, China; Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Nanjing 210023, Jiangsu, China. Electronic address: liwaii@126.com.
authors.forename: Wei
authors.initials: W
authors.lastname: Li
authors.affiliation: School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing 210023, Jiangsu, China. Electronic address: cpuwtl@gmail.com.
authors.forename: Tian-Lin
authors.initials: TL
authors.lastname: Wang
authors.affiliation: School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing 210023, Jiangsu, China.
authors.forename: Hong-Mei
authors.initials: HM
authors.lastname: Wen
authors.affiliation: School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing 210023, Jiangsu, China.
authors.forename: Long
authors.initials: L
authors.lastname: Chen
authors.affiliation: School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing 210023, Jiangsu, China.
authors.forename: Jian
authors.initials: J
authors.lastname: Liu
mesh_terms: D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D002316:Cardiotonic Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D006333:Heart Failure / Q000188:drug therapy; D006339:Heart Rate / Q000187:drug effects; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D011719:Pyrazines / Q000138:chemical synthesis / Q000378:metabolism* / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: C572935:2,5-dihydroxymethyl-3,6-dimethylpyrazine; D002316:Cardiotonic Agents; D011719:Pyrazines
keywords: Heart failure; Liguzinediol; Metabolite; Synthesis