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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

Dimensions Citations:

Plum Analytics:
Number of Figures: 5
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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 (using NLM MeSH Indexing)
Animals -
Anticholesteremic Agents - chemical synthesis
Anticholesteremic Agents - pharmacology
Azetidines - chemical synthesis
Azetidines - pharmacology
Biological Transport - drug effects
Cell Survival - drug effects
Cholesterol - metabolism
Cholesterol - pharmacokinetics
Dogs -
Ezetimibe - analogs & derivatives
Ezetimibe - chemical synthesis
Ezetimibe - pharmacology
Hep G2 Cells -
Humans -
Intestinal Absorption - drug effects
Intestine, Small - drug effects
Intestine, Small - metabolism
Liver - drug effects
Liver - metabolism
Madin Darby Canine Kidney Cells -
Mice -
Structure-Activity Relationship -
Tritium -
beta-Lactams - chemical synthesis
beta-Lactams - pharmacology

Find related publications in this database (Keywords)
Cholesterol absorption inhibitor
Cardiovascular heart disease
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