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3 results on '"Christina Kiziridi"'

1. Synthesis of chroman analogues of lipoic acid and evaluation of their activity against reperfusion arrhythmias

Author

Christina Kiziridi, Theodora Calogeropoulou, Panos N. Kourounakis, Catherine Gaitanaki, Maria Koufaki, Elissavet Theodorou, Anastasia Detsi, Panagiota Papazafiri, Athanasios Vassilopoulos, Angeliki P. Kourounakis, and Eleni A. Rekka

Subjects
Male, Antioxidant, Stereochemistry, medicine.medical_treatment, Clinical Biochemistry, Drug Evaluation, Preclinical, Pharmaceutical Science, Myocardial Reperfusion Injury, Biochemistry, Chemical synthesis, Lipid peroxidation, chemistry.chemical_compound, Drug Discovery, medicine, Animals, Peptide bond, Phenols, Chromans, Rats, Wistar, Molecular Biology, Thioctic Acid, Vitamin E, Organic Chemistry, Arrhythmias, Cardiac, Rats, Lipoic acid, chemistry, Molecular Medicine, lipids (amino acids, peptides, and proteins), Trolox
Abstract

Novel hybrids of lipoic acid and trolox connected through triamine spacers as well as analogues in which the lipoic acid was attached at different positions of the chroman moiety of vitamin E through an amide bond, were synthesized and exhibited strong inhibition of the microsomal lipid peroxidation. Moreover, the new molecules, at 1 microM concentration, reduced reperfusion arrhythmias and MDA content on isolated rat heart preparations, with the 2- and 5-subtituted chromans possessing the better cardioprotective activity.

Published
2004
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2. Design and synthesis of 1,2-dithiolane derivatives and evaluation of their neuroprotective activity

Author

Christina Kiziridi, Faidra Nikoloudaki, Maria Koufaki, and Michael N. Alexis

Subjects
Thioctic Acid, Stereochemistry, Organic Chemistry, Clinical Biochemistry, Triazole, Drug Evaluation, Preclinical, Pharmaceutical Science, Biological activity, Biochemistry, Chemical synthesis, Hippocampus, Dithiolane, Cell Line, chemistry.chemical_compound, Neuroprotective Agents, chemistry, Amide, Drug Discovery, Molecular Medicine, Tetrazole, Bioisostere, Thiazole, Molecular Biology
Abstract

We designed and synthesized new analogues containing 1,2-dithiolane-3-alkyl and protected or free catechol moieties connected through heteroaromatic rings such as triazole, 1,2,4-oxadiazole, 1,3,4-oxadiazole, tetrazole or thiazole in order to explore the influence of the bioisosteric replacement of the amide group on the neuroprotective activity of the lipoic acid/dopamine conjugate. Evaluation of the activity of the new compounds, using glutamate-challenged hippocampal HT22 cells, showed that incorporation of heteroaromatic rings in the alkyl-1,2-dithiolane moieties in conjunction with another antioxidant, in this case catechol, may result in strong neuroprotective activity.

Published
2009

3. Synthesis and biological evaluation of benzopyran analogues bearing class III antiarrhythmic pharmacophores

Author

Athanasios Vassilopoulos, Panagiota Papazafiri, Maria Koufaki, Zsolt Ákos Nagy, Christina Kiziridi, Attila S. Farkas, András Varró, and Alexandros Makriyannis

Subjects
Male, Cardiac Complexes, Premature, Tertiary amine, Stereochemistry, medicine.medical_treatment, Clinical Biochemistry, Myocardial Ischemia, Pharmaceutical Science, Action Potentials, Myocardial Reperfusion Injury, Antiarrhythmic agent, In Vitro Techniques, Biochemistry, Chemical synthesis, Antioxidants, Rats, Sprague-Dawley, chemistry.chemical_compound, Electrocardiography, Drug Discovery, medicine, Animals, Benzopyrans, Mode of action, Molecular Biology, chemistry.chemical_classification, Methylamine, Organic Chemistry, Heart, Sulfonamide, Benzopyran, Rats, chemistry, Mechanism of action, Molecular Medicine, Rabbits, medicine.symptom, Anti-Arrhythmia Agents, Microelectrodes
Abstract

We have synthesized a series of compounds combining the hydroxy-benzopyran ring of vitamin E with the methylsulfonylaminophenyl group of class III antiarrhythmic drugs, connected through tertiary amine moieties. Evaluation of the antiarrhythmic and antioxidant activity of the new compounds was carried out on isolated rat heart preparations using the non-recirculating Langendorff mode. The new analogues were present, at 10 microM concentration, during ischemia and reperfusion. Selected compounds were further studied by a conventional microelectrode method in order to get insight into their cellular mode of action. The most active compound, N-[4-[2-[[2-(3,4-dihydro-6-hydroxy-2,2,7,8-tetramethyl-2H-1-benzopyran-5-yl)ethyl] methylamine]ethyl]phenyl]methanesulfonamide (19a), reduces premature beats, prolongs QT and QRS intervals during ischemia and reperfusion, and reduces MDA content, leading to a fast recovery of the heart. In addition, it exhibits moderate class III antiarrhythmic action.

Published
2006

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