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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
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Molecules 2013, 18(4), 4561-4572; https://doi.org/10.3390/molecules18044561
Received: 15 March 2013 / Revised: 8 April 2013 / Accepted: 11 April 2013 / Published: 18 April 2013
(This article belongs to the Section Medicinal Chemistry)
Liguzinediol (LZDO) ester prodrugs 35 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 35 were found to display a potent positive inotropic effect on the myocardium, without the risk of arrhythmia. Prodrugs 35 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. View Full-Text
Keywords: liguzinediol; liguzinediol prodrugs; synthesis; positive inotropic effect; pharmacokinetics 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. https://doi.org/10.3390/molecules18044561

AMA 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(4):4561-4572. https://doi.org/10.3390/molecules18044561

Chicago/Turabian Style

Liu, Zheng, Wei Li, Hong-Mei Wen, Hui-Min Bian, Jing Zhang, Lei Chen, Long Chen, and Kun-Di Yang. 2013. "Synthesis, Biological Evaluation, and Pharmacokinetic Study of Novel Liguzinediol Prodrugs" Molecules 18, no. 4: 4561-4572. https://doi.org/10.3390/molecules18044561

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