Search

Your search keyword '"Henryk Marona"' showing total 4 results
Start Over Author "Henryk Marona" Journal bioorganicmedicinal chemistry
4 results on '"Henryk Marona"'

1. Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH

Author

Agnieszka, Gunia-Krzyżak, Dorota, Żelaszczyk, Anna, Rapacz, Ewa, Żesławska, Anna M, Waszkielewicz, Katarzyna, Pańczyk, Karolina, Słoczyńska, Elżbieta, Pękala, Wojciech, Nitek, Barbara, Filipek, and Henryk, Marona

Subjects
Models, Molecular, Disease Models, Animal, Electroshock, Mice, Structure-Activity Relationship, Dose-Response Relationship, Drug, Molecular Structure, Seizures, Animals, Anticonvulsants, Crystallography, X-Ray, Amino Alcohols, Rats
Abstract

A series of twenty two (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH

Published
2016

2. Anticonvulsant evaluation of aminoalkanol derivatives of 2- and 4-methylxanthone

Author

Henryk Marona, Agnieszka Gunia, Edward Szneler, Marek T. Cegla, Anna M. Waszkielewicz, Lucyna Antkiewicz-Michaluk, and Natalia Szkaradek

Subjects
synthesis, medicine.medical_treatment, Xanthones, Clinical Biochemistry, Pharmaceutical Science, Pharmacology, Biochemistry, Xanthone Derivatives, chemistry.chemical_compound, Mice, Structure-Activity Relationship, Seizures, neurotoxicity, Drug Discovery, Xanthone, medicine, Animals, Molecular Biology, Neurons, Electroshock, Organic Chemistry, Neurotoxicity, medicine.disease, Maximal electroshock, Anticonvulsant, chemistry, xanthone, MES, Molecular Medicine, Pentylenetetrazole, Anticonvulsants, Calcium Channels, anticonvulsant, Injections, Intraperitoneal
Abstract

A series of 17 new aminoalkanol derivatives of 6-methoxy- or 7-chloro-2-methylxanthone as well as 6-methoxy-4-methylxanthone was synthesized and evaluated for anticonvulsant activity. All compounds were verified in mice after intraperitoneal (ip) administration in maximal electroshock (MES) and subcutaneous pentetrazole (scMet) induced seizures as well as neurotoxicity assessment. Eleven of the tested substances showed protection against electrically evoked seizures in the majority of the tested mice at the dose of 100 mg/kg. Additionally, one was effective at the dose of 30 mg/kg. Five substances were active at the dose of 300 mg/kg or at the dose of 100 mg/kg in the minority of the tested mice. The most promising compound revealed ED(50) value of 47.57 mg/kg in MES (mice, ip, 1h after administration) and at the same time its TD(50) was evaluated as above 400 mg/kg. Those values gave PI (calculated as TD(50)/ED(50)) of more than 8.41. Three other synthesized xanthone derivatives also proved to act as anticonvulsants and showed ED(50) values in MES test (mice, ip) ranged 80-110 mg/kg. Results were quite encouraging and suggested that in the group of xanthone derivatives new potential anticonvulsants might be found.

Published
2012

3. Preliminary evaluation of pharmacological properties of some xanthone derivatives

Author

Barbara Filipek, Edward Szneler, Henryk Marona, Marek T. Cegla, Natalia Szkaradek, Anna Rapacz, Małgorzata Dybała, and Agata Siwek

Subjects
Male, Stereochemistry, medicine.medical_treatment, Xanthones, Clinical Biochemistry, Pharmaceutical Science, Adrenergic, Pharmacology, Antiarrhythmic agent, Biochemistry, Chemical synthesis, Xanthone Derivatives, antiarrhythmic, Electrocardiography, Mice, Receptors, Adrenergic, alpha-2, Seizures, Receptors, Adrenergic, alpha-1, Drug Discovery, hypotensive and anticonvulsive activities, Radioligand, medicine, Animals, xanthones, Rats, Wistar, Molecular Biology, Antihypertensive Agents, Chemistry, radioligand-binding assay, Organic Chemistry, Biological activity, Adrenergic alpha-2 Receptor Antagonists, Ligand (biochemistry), Rats, Kinetics, Anticonvulsant, Adrenergic alpha-1 Receptor Antagonists, Molecular Medicine, Anticonvulsants, Anti-Arrhythmia Agents
Abstract

A series of xanthone derivatives were synthesized and examined for electrocardiographic, antiarrhythmic, hypotensive and anticonvulsant activities as well as for alpha(1)- and beta(1)-adrenergic binding affinities. Among the investigated compounds, some of them exhibited significant antiarrhythmic and/or hypotensive activity. The data obtained via receptor binding assay are in agreement with pharmacological results and could explain antiarrhythmic and/or hypotensive activity of the newly synthesized structures.

Published
2008

4. Anticonvulsant activity of some xanthone derivatives

Author

Maria Walczak, Lucyna Antkiewicz-Michaluk, Edward Szneler, Henryk Marona, and Elżbieta Pękala

Subjects
Phenytoin, medicine.drug_class, Stereochemistry, anticonvulsive activities, medicine.medical_treatment, Xanthones, Clinical Biochemistry, Pharmaceutical Science, Biochemistry, chemistry.chemical_compound, Mice, Seizures, Drug Discovery, Xanthone, medicine, Animals, xanthones, Molecular Biology, Benzodiazepine, Electroshock, Dose-Response Relationship, Drug, Molecular Structure, radioligand-binding assay, Organic Chemistry, Biological activity, Carbamazepine, enantiopurity, Rats, Anticonvulsant, chemistry, Lipophilicity, Molecular Medicine, Pentylenetetrazole, Anticonvulsants, Enantiomer, medicine.drug
Abstract

A series of appropriate alkanolamine and amide derivatives of xanthone were prepared and evaluated for anticonvulsant activity using maximal electroshock (MES) and subcutaneous pentylenetetrazole (scMet) induced seizures, and for neurotoxicity (TOX) using the rotorod test on mice and rats. The most promising compounds seem to be the appropriate aminoalkanolic derivatives of 6-chloroxanthone, among which the R-(-) and S-(+)-2amino-1-propanol derivatives of 6-chloro-2-methylxanthone (2(a) and 2(b)) displayed anti-MES activity (in mice) with a protective index (TD(50)/ED(50)) of 6.23

Published
2008

Catalog

Books, media, physical & digital resources
See catalog results