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

Synthesis, Biological Evaluation, and Pharmacokinetic Study of Novel Liguzinediol Prodrugs

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Received: 15 March 2013; in revised form: 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.
Keywords: liguzinediol; liguzinediol prodrugs; synthesis; positive inotropic effect; pharmacokinetics
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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.

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.

Chicago/Turabian Style

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.


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