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Molecules 2013, 18(4), 4561-4572; https://doi.org/10.3390/molecules18044561

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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Received: 15 March 2013 / Revised: 8 April 2013 / Accepted: 11 April 2013 / Published: 18 April 2013
(This article belongs to the Section Medicinal Chemistry)
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Abstract

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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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.

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