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Synthesis, Biological Evaluation, and Pharmacokinetic Study of Novel Liguzinediol Prodrugs
School of Pharmacy, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing 210046, Jiangsu, China
* Author to whom correspondence should be addressed.
Received: 15 March 2013; in revised form: 8 April 2013 / Accepted: 11 April 2013 / Published: 18 April 2013
Abstract: Liguzinediol (LZDO) ester prodrugs 3–5 were synthesized and evaluated in vitro and in vivo for their potential use in prolonging the half-life of the parent drug LZDO (1a) in vivo. Prodrugs 3–5 were found to display a potent positive inotropic effect on the myocardium, without the risk of arrhythmia. Prodrugs 3–5 rapidly underwent enzymatic hydrolysis to release the parent compound LZDO in 1–3 h in rat liver microsomes and rat plasma. The half-life of the parent compound was prolonged after intragastric administration of prodrug 3, which was found to be a superior prodrug candidate for increasing myocardial contractility.
Keywords: liguzinediol; liguzinediol prodrugs; synthesis; positive inotropic effect; pharmacokinetics
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MDPI and ACS Style
Liu, Z.; Li, W.; Wen, H.-M.; Bian, H.-M.; Zhang, J.; Chen, L.; Chen, L.; Yang, K.-D. Synthesis, Biological Evaluation, and Pharmacokinetic Study of Novel Liguzinediol Prodrugs. Molecules 2013, 18, 4561-4572.
Liu Z, Li W, Wen H-M, Bian H-M, Zhang J, Chen L, Chen L, Yang K-D. Synthesis, Biological Evaluation, and Pharmacokinetic Study of Novel Liguzinediol Prodrugs. Molecules. 2013; 18(4):4561-4572.
Liu, Zheng; Li, Wei; Wen, Hong-Mei; Bian, Hui-Min; Zhang, Jing; Chen, Lei; Chen, Long; Yang, Kun-Di. 2013. "Synthesis, Biological Evaluation, and Pharmacokinetic Study of Novel Liguzinediol Prodrugs." Molecules 18, no. 4: 4561-4572.