- Fluorinated dual antithrombotic compounds based on 1,4-benzoxazine scaffold
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Fluorinated 3,4-dihydro-2H-1,4-benzoxazine derivatives possessing both thrombin inhibitory and glycoprotein IIb/IIIa receptor antagonistic activities were prepared as potential dual antithrombotic compounds. Fluorine scan (3-fluorobenzyl, 4-fluorobenzyl,
- Ili?, Milo?,Kikelj, Danijel,Ila?, Janez
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scheme or table
p. 255 - 263
(2012/07/28)
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- Thrombin inhibitors with lipid peroxidation and lipoxygenase inhibitory activities
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Vascular oxidative stress, endothelial injury, and thrombosis are intertwined processes that display a synergistic pathological effect in many cardiovascular diseases. Antithrombotic therapy with anticoagulant and/or antiplatelet agents, combined with interventions against vascular oxidative stress and/or inflammation, both boosting endothelial antithrombotic potential, could display a synergistic action in the treatment of thrombosis. Of the compounds 10a-h and 11a-d, shown to possess thrombin inhibitory activity, 11a-d were found to display radical scavenging activity, 10a, 10d, and 10f were demonstrated to inhibit lipid peroxidation of linoleic acid, and 10b and 10h inhibited soybean lipoxygenase. The observed combination of thrombin inhibition with lipid peroxidation and/or lipoxygenase inhibitory activity makes compounds 10 and 11 interesting candidates for further investigations towards multiple antithrombotic drugs.
- Ilic, Milos,Kontogiorgis, Christos,Hadjipavlou-Litina, Dimitra,Ilas, Janez,Kikelj, Danijel
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scheme or table
p. 4705 - 4709
(2011/09/20)
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- Synthesis and antiproliferative activity of 2-(([1,2,4]triazolo[4,3-b]- pyridazin-6-yloxy)methyl)-2,4-dimethyl-3,4-dihydro-2Hbenzo[b][1,4]oxazine derivatives
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A small library of [1,2,4]triazolo[4,3-b]pyridazin-6-yloxy derivatives 14-17 of N-benzyl-N-(2-((4-amidinophenoxy)methyl)-2,4-dimethyl-3,4-dihydro-2H- benzo[b][1,4]oxazin-7-yl)-oxalic acid monoamides 1 was prepared by replacement of benzamidine with a [1,2
- Ilic, Milos,Ilas, Janez,Liekens, Sandra,Matyus, Peter,Kikelj, Danijel
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scheme or table
p. 298 - 311
(2011/12/15)
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- Design and synthesis of novel platelet fibrinogen receptor antagonists with 2H-1,4-benzoxazine-3(4H)-one scaffold. A systematic study
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New platelet glycoprotein IIb/IIIa (GP IIb/IIIa, integrin αIIbβ3) antagonists were prepared on a 2H-1,4-benzoxazine-3(4H)-one scaffold. Their anti-aggregatory activities in human platelet rich plasma and their affinity towards α sub
- Anderluh, Marko,Cesar, Jǒko,?tefanǐ, Petra,Kikelj, Danijel,Janě, Damjan,Murn, Jernej,Nadrah, Kristina,Tominc, Mojca,Addicks, Elisabeth,Giannis, Athanassios,Stegnar, Mojca,Dolenc, Marija Sollner
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- Conformationally tailored N-[(2-methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)carbonyl]proline templates as molecular tools for the design of peptidomimetics. Design and synthesis of fibrinogen receptor antagonists.
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The proline peptide bond was shown by 2D proton NMR studies to exist exclusively in the trans conformation in benzyl (2S)-1-[[(2S)-2-methyl-6-nitro-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl]carbonyl]-2-pyrrolidinecarboxylate [(S,S)-11], benzyl (2S)-1-[[(2S
- Stefanic, Petra,Simoncic, Zvone,Breznik, Matej,Plavec, Janez,Anderluh, Marko,Addicks, Elisabeth,Giannis, Athanassios,Kikelj, Danijel
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p. 1511 - 1517
(2007/10/03)
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