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Dive into the research topics where Jerzy Kossakowski is active.

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Featured researches published by Jerzy Kossakowski.


Farmaco | 2001

Synthesis of new N-substituted cyclic imides with an expected anxiolytic activity. XVII. Derivatives of 1-ethoxybicyclo[2.2.2]-oct-5-one-2,3-dicarboximide

Jerzy Kossakowski; Monika Jarocka

The preparation of a number of derivatives of 1-ethoxybicyclo[2.2.2]-oct-5-one-2,3-dicarboximide with potential anxiolytic activity has been described. The aim of our study was to obtain new analogs of tandospirone.


Molecules | 2010

Synthesis and preliminary evaluation of the antimicrobial activity of selected 3-benzofurancarboxylic acid derivatives.

Jerzy Kossakowski; Mariola Krawiecka; Bożena Kuran; Joanna Stefańska; Irena Wolska

Halogen derivatives of selected 3-benzofurancarboxylic acids were prepared using 6-acetyl-5-hydroxy-2-methyl-3-benzofuranocarboxylic acid as starting material. 1H-NMR spectra were obtained for all of the synthesized structures, and for compound VI, an X-ray crystal structure was also obtained. All derivatives were tested for antimicrobial activity against a selection of Gram-positive cocci, Gram-negative rods and yeasts. Three compounds, III, IV, and VI, showed antimicrobial activity against Gram-positive bacteria (MIC 50 to 200 μg/mL). Compounds VI and III exhibited antifungal activity against the Candida strains C. albicans and C. parapsilosis (MIC – 100 μg/mL).


Molecules | 2008

4-Azatricyclo[5.2.2.02,6]undecane-3,5,8-triones as Potential Pharmacological Agents

Jerzy Kossakowski; Anna Bielenica; Barbara Miroslaw; Anna E. Koziol; Izabela Dybała; Marta Struga

A series of twenty six arylpiperazine and aminoalkanol derivatives of 4-aza-tricyclo[5.2.2.02,6]undecane-3,5,8-trione have been prepared. The synthesized compounds were evaluated for their cytotoxicity and anti-HIV-1 activity in MT-4 cells.


Molecules | 2009

Synthesis and Evaluation of in Vitro Biological Activity of 4-Substituted Arylpiperazine Derivatives of 1,7,8,9-Tetrachloro- 10,10-dimethoxy-4-azatricyclo(5.2.1.0 2,6 )dec-8-ene-3,5-dione

Jerzy Kossakowski; Magdalena Pakosinska-Parys; Marta Struga; Izabela Dybała; Anna E. Koziol; Paolo La Colla; Laura Ester Marongiu; Cristina Ibba; David Collu; Roberta Loddo

A series of twenty arylpiperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione have been prepared. These derivatives were tested in vitro with the aim of identifying novel lead compounds active against emergent and re-emergent human and cattle infectious diseases (AIDS, hepatitis B and C, tuberculosis, bovine viral diarrhea). In particular, these compounds were evaluated in vitro against representatives of different virus classes, such as a HIV-1 (Retrovirus), a HBV (Hepadnavirus) and the single-stranded RNA+ viruses Yellow fever virus (YFV) and Bovine viral diarrhea virus (BVDV), both belonging to the Flaviridae. Compounds 2c, 2g and 3d showed a modest activity against CVB-2. The molecular structures of the starting imide 1 and one of propyl-piperazine derivatives, 3b, have been determined by an X-ray crystallography study.


Journal of Pharmacology and Experimental Therapeutics | 2012

Synthesis and Antifungal Activity of Derivatives of 2- and 3-Benzofurancarboxylic Acids

Elżbieta Hejchman; Kinga Ostrowska; Dorota Maciejewska; Jerzy Kossakowski; William E. Courchesne

We found that amiodarone has potent antifungal activity against a broad range of fungi, potentially defining a new class of antimycotics. Investigations into its molecular mechanisms showed amiodarone mobilized intracellular Ca2+, which is thought to be an important antifungal characteristic of its fungicidal activity. Amiodarone is a synthetic drug based on the benzofuran ring system, which is contained in numerous compounds that are both synthetic and isolated from natural sources with antifungal activity. To define the structural components responsible for antifungal activity, we synthesized a series of benzofuran derivatives and tested them for the inhibition of growth of two pathogenic fungi, Cryptococcus neoformans and Aspergillus fumigatus, to find new compounds with antifungal activity. We found several derivatives that inhibited fungal growth, two of which had significant antifungal activity. We were surprised to find that calcium fluxes in cells treated with these derivatives did not correlate directly with their antifungal effects; however, the derivatives did augment the amiodarone-elicited calcium flux into the cytoplasm. We conclude that antifungal activity of these new compounds includes changes in cytoplasmic calcium concentration. Analyses of these benzofuran derivatives suggest that certain structural features are important for antifungal activity. Antifungal activity drastically increased on converting methyl 7-acetyl-6-hydroxy-3-methyl-2-benzofurancarboxylate (2b) into its dibromo derivative, methyl 7-acetyl-5-bromo-6-hydroxy-3-bromomethyl-2-benzofurancarboxylate (4).


Archives of Pharmacal Research | 2010

Synthesis and microbiological activity of thiourea derivatives of 4-azatricyclo[5.2.2.0(2,6)]undec-8-ene-3,5-dione.

Marta Struga; Szymon Rosolowski; Jerzy Kossakowski; Joanna Stefańska

A series of thiourea derivatives of 4-azatricyclo[5.2.2.02,6]undec-8-ene-3,5-dione were synthesized. The compounds were investigated for antibacterial activity, including Gram-positive cocci, Gram-negative rods, and antifungal activity. Compounds 1b, 2b, 4b showed significant inhibition against Gram-positive cocci. Research was carried out over 10 standard strains and 20 hospital strains. Synthesized compounds were evaluated for their cytotoxicity and anti-HIV-1 activity in MT-4 cells.


Annals of Microbiology | 2010

Antimicrobial activity of 10-(diphenylmethylene)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives

Joanna Stefańska; Anna Bielenica; Marta Struga; Stefan Tyski; Jerzy Kossakowski; Paolo La Colla; Elena Tamburini; Roberta Loddo

Antibacterial and antifungal activity of 10-(diphenylmethylene)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives were examined by the disk diffusion method (growth inhibition zone diameter in agar medium). The minimal inhibitory concentrations (MICs) for the most active agents were determined. Title compounds were also evaluated in vitro against HIV-1 virus and their cytotoxicity was determined. Aminoalkanol derivatives exhibited activity against the majority of microorganisms studied.


Medicinal Chemistry Research | 2011

Biological evaluation of novel 1,4-dithiine derivatives as potential antimicrobial agents

Anna Bielenica; Jerzy Kossakowski; Marta Struga; Izabela Dybała; Paolo La Colla; Elena Tamburini; Roberta Loddo

The preparation of twelve aminoalkanol derivatives of 2,3-dihydro-5H-[1,4]dithiino[2,3-c]pyrrole-5,7(6H)-dione was described. Newly obtained compounds, as well as their propyl and butyl analogues, were evaluated in vitro against selected viruses. Selected derivatives were tested for their antibacterial and antifungal activity. Compounds 3h, 3j, 4b and 5a–d showed moderate to significant protections against CVB-2, HSV-1 and YFV viruses. The molecular structures of 4a, 5c and 5g were determined by an X-ray analysis.


Medicinal Chemistry Research | 2009

Synthesis of new derivatives of 2,2-dimethyl-2,3-dihydro-7-benzo[b]furanol with potential antimicrobial activity

Jerzy Kossakowski; Kinga Ostrowska; Marta Struga; Joanna Stefańska

A series of 13 new ether-linked derivatives of 2,2-dimethyl-2,3-dihydro-7-benzo[b]furanol have been designed and synthesized. Ten of them were evaluated for their potential antimicrobial activity against some Gram-positive and Gram-Negative bacteria and fungi of the Candida species.


Central European Journal of Biology | 2009

Biological evaluation of 10-(diphenylmethylene)- 4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives

Joanna Stefańska; Anna Bielenica; Marta Struga; Stafan Tyski; Jerzy Kossakowski; Roberta Loddo; Cristina Ibba; David Collu; Esther Marongiu; Paolo La Colla

Antibacterial and antifungal activity of 10-(diphenylmethylene)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives were examined by the disc-diffusion method (growth inhibition zone diameter in agar medium). The MIC’s for the most active agents were determined. Title compounds were also evaluated in vitro against representatives of different virus classes. Most of the tested compounds exhibit activity against CVB-2 virus.

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Marta Struga

Medical University of Warsaw

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Mariola Krawiecka

Medical University of Warsaw

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Anna E. Koziol

Maria Curie-Skłodowska University

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Joanna Stefańska

Medical University of Warsaw

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Anna Bielenica

Medical University of Warsaw

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Kinga Ostrowska

Medical University of Warsaw

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Aleksandra Drzewiecka

Maria Curie-Skłodowska University

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