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Synthesis and evaluation of novel amide amino-β-lactam derivatives as cholesterol absorption inhibitors (CROSBI ID 218233)

Prilog u časopisu | izvorni znanstveni rad | međunarodna recenzija

Dražić, Tonko ; Sachdev, Vinay ; Leopold, Christina ; Patankar, Jay V. ; Malnar, Martina ; Hećimović, Silva ; Levak-Frank, Sanja ; Habuš, Ivan ; Kratky, Dagmar Synthesis and evaluation of novel amide amino-β-lactam derivatives as cholesterol absorption inhibitors // Bioorganic & medicinal chemistry, 23 (2015), 10; 2353-2359. doi: 10.1016/j.bmc.2015.03.067

Podaci o odgovornosti

Dražić, Tonko ; Sachdev, Vinay ; Leopold, Christina ; Patankar, Jay V. ; Malnar, Martina ; Hećimović, Silva ; Levak-Frank, Sanja ; Habuš, Ivan ; Kratky, Dagmar

engleski

Synthesis and evaluation of novel amide amino-β-lactam derivatives as cholesterol absorption inhibitors

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.

β-Lactam; Cholesterol absorption inhibitor; Hyperlipidemia; Cardiovascular heart disease

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Podaci o izdanju

23 (10)

2015.

2353-2359

objavljeno

0968-0896

10.1016/j.bmc.2015.03.067

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Kemija

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