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6 results on '"Grzonek A"'

1. Synthesis of Novel Pyrido[4,3-e][1,2,4]triazino[3,2-c][1,2,4]thiadiazine 6,6-dioxide Derivatives with Potential Anticancer Activity

Author

Jarosław Sławiński, Aleksandra Grzonek, Beata Żołnowska, and Anna Kawiak

Subjects
pyrido[4,3-e][1,2,4]triazino[3,2-c][1,2,4]thiadiazine, 6,6-dioxides, synthesis, NMR studies, cytotoxic activity, Organic chemistry, QD241-441
Abstract

A series of novel 3-/2,3-substituted pyrido[4,3-e][1,2,4]triazino[3,2-c][1,2,4]thiadiazine 6,6-dioxides 4–28 have been synthesized by the reaction of 3-amino-2-(4-thioxo-1,4-dihydropyridin-3-yl-sulfonyl)guanidine with either 2-oxoalkanoic acids and its esters, or phenylglyoxylic hydrates in glacial acetic acid. Some of them exhibited reasonable or moderate anticancer activity toward human cancer cell lines, HCT-116, MCF-7 and HeLa. The structure of this novel heterocyclic ring system was confirmed by 1D-NMR and 2D-NMR spectroscopic data including COSY, ROESY and HMBC, elemental analyses and MS spectrometry.

Published
2015
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2. N-Substituted N'-(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)guanidines--Antibacterial, Cytotoxic Activities and Some Structure-Activity Relationships

Author

Beata, Zołnowska, Jarosław, Sławiński, Aleksandra, Grzonek, Anna, Kędzia, Ewa, Kwapisz, and Anna, Kawiak

Subjects
Structure-Activity Relationship, Bacteria, Humans, Bacterial Infections, Microbial Sensitivity Tests, Guanidines, Anti-Bacterial Agents
Abstract

A series of N-substituted N'-(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)guanidine derivatives bearing sulfonamide moiety have been screened in vitro for antibacterial activity against isolates from patients with infections of oral cavity, respiratory tract and intestinal tract. The majority of compounds exhibited good antibacterial potency. 1-[4-Chloro-5-methyl-2-(4-trifluoromethylbenzylthio)benzenesulfonyl]-3-(3-sulfamoylphenyl)guanidine (13) showed very strong activity, with MIC ≤ 6.2 μg/ml against eleven bacteria strains belonged to Gram-positive anaerobes and aerobes. Furthermore, compound 13 exhibited promising activity toward highly resistant microorganisms such as methicillin-resistant Staphylococcus aureus and Enterococcusfaecalis. It was found that Parvimonas micra, Finegoldia magna, Peptostreptococcus anaerobius, Propionibacterium acnes showed the highest susceptibility toward the investigated guanidines.

Published
2015

5. Synthesis of Novel Pyrido[4,3-e][1,2,4]triazino[3,2-c][1,2,4] thiadiazine 6,6-dioxide Derivatives with Potential Anticancer Activity.

Author

Sławiński, Jarosław, Grzonek, Aleksandra, Żołnowska, Beata, and Kawiak, Anna

Subjects
*ANTINEOPLASTIC agents, *CANCER cells, *CELL lines, *PHENYLGLYOXYLIC acid, *ACETIC acid, *PHYSIOLOGY
Abstract

A series of novel 3-/2,3-substituted pyrido[4,3-e][1,2,4]triazino[3,2-c][1,2,4]thiadiazine 6,6-dioxides 4-28 have been synthesized by the reaction of 3-amino-2-(4-thioxo-1,4-dihydrop yridin-3-yl-sulfonyl)guanidine with either 2-oxoalkanoic acids and its esters, or phenylglyoxylic hydrates in glacial acetic acid. Some of them exhibited reasonable or moderate anticancer activity toward human cancer cell lines, HCT-116, MCF-7 and HeLa. The structure of this novel heterocyclic ring system was confirmed by 1D-NMR and 2D-NMR spectroscopic data including COSY, ROESY and HMBC, elemental analyses and MS spectrometry. [ABSTRACT FROM AUTHOR]

Published
2016
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6. N-Substituted N' -(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)guanidines - Antibacterial, cytotoxic activities and some structure-activity relationships

Author

Ewa Kwapisz, Beata Zolnowska, Aleksandra Grzonek, Jarosław Sławiński, Anna Kędzia, and Anna Kawiak

Subjects
Microbiology (medical), biology, ved/biology, Peptostreptococcus anaerobius, ved/biology.organism_classification_rank.species, General Medicine, medicine.disease_cause, biology.organism_classification, Applied Microbiology and Biotechnology, Microbiology, chemistry.chemical_compound, Propionibacterium acnes, chemistry, Staphylococcus aureus, medicine, Potency, Guanidine, Parvimonas micra, Antibacterial activity, Bacteria
Abstract

A series of N-substituted N'-(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)guanidine derivatives bearing sulfonamide moiety have been screened in vitro for antibacterial activity against isolates from patients with infections of oral cavity, respiratory tract and intestinal tract. The majority of compounds exhibited good antibacterial potency. 1-[4-Chloro-5-methyl-2-(4-trifluoromethylbenzylthio)benzenesulfonyl]-3-(3-sulfamoylphenyl)guanidine (13) showed very strong activity, with MIC ≤ 6.2 μg/ml against eleven bacteria strains belonged to Gram-positive anaerobes and aerobes. Furthermore, compound 13 exhibited promising activity toward highly resistant microorganisms such as methicillin-resistant Staphylococcus aureus and Enterococcus faecalis. It was found that Parvimonas micra, Finegoldia magna, Peptostreptococcus anaerobius, Propionibacterium acnes showed the highest susceptibility toward the investigated guanidines.

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