Next Article in Journal
Triacylglyceride, Antioxidant and Antimicrobial Features of Virgin Camellia oleifera, C. reticulata and C. sasanqua Oils
Previous Article in Journal
Deuterium Isotope Effects on 13C-NMR Chemical Shifts of 10-Hydroxybenzo[h]quinolines
Molecules 2013, 18(4), 4561-4572; doi:10.3390/molecules18044561
Article

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

, * , , , , ,  and
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 / Revised: 8 April 2013 / Accepted: 11 April 2013 / Published: 18 April 2013
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [275 KB, uploaded 18 June 2014]   |   Browse Figures
SciFeed

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 liguzinediol; liguzinediol prodrugs; synthesis; positive inotropic effect; pharmacokinetics
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

Supplementary material

Share & Cite This Article

Further Mendeley | CiteULike
Export to BibTeX |
EndNote |
RIS
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.

View more citation formats

Related Articles

Article Metrics

For more information on the journal, click here

Comments

[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert