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SHR Neuro Krebs Kardio Lipid

Dražić, T; Sachdev, V; Leopold, C; Patankar, JV; Malnar, M; Hećimović, S; Levak-Frank, S; Habuš, I; Kratky, D.
Synthesis and evaluation of novel amide amino-β-lactam derivatives as cholesterol absorption inhibitors.
Bioorg Med Chem. 2015; 23(10): 2353-2359. [OPEN ACCESS]
Web of Science PubMed PUBMED Central FullText FullText_MUG

 

Autor/innen der Med Uni Graz:
Kratky Dagmar
Leopold Christina
Levak Sanja
Sachdev Vinay
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Number of Figures: 5
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Abstract:
The β-lactam cholesterol absorption inhibitor ezetimibe is so far the only representative of this class of compounds on the market today. The goal of this work was to synthesize new amide ezetimibe analogs from trans-3-amino-(3R,4R)-β-lactam and to test their cytotoxicity and activity as cholesterol absorption inhibitors. We synthesized six new amide ezetimibe analogs. All new compounds exhibited low toxicity in MDCKIIwt, hNPC1L1/MDCKII and HepG2 cell lines and showed significant inhibition of cholesterol uptake in hNPC1L1/MDCKII cells. In addition, we determined the activity of the three compounds to inhibit cholesterol absorption in vivo. Our results demonstrate that these compounds considerably reduce cholesterol concentrations in liver and small intestine of mice. Thus, our newly synthesized amide ezetimibe analogs are cholesterol absorption inhibitors in vitro and in vivo. Copyright © 2015 The Authors. Published by Elsevier Ltd.. All rights reserved.

Find related publications in this database (Keywords)
beta-Lactam
Cholesterol absorption inhibitor
Hyperlipidemia
Cardiovascular heart disease
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