Výsledky vyhledávání - "Sebastian Demkowicz"

Akademický článek

Convenient and efficient N-methylation of secondary amines under solvent-free ball milling conditions

Autor: Mikołaj Walter, Olga Ciupak, Karol Biernacki, Janusz Rachoń, Dariusz Witt, Sebastian Demkowicz

Publikováno v: Scientific Reports, Vol 14, Iss 1, Pp 1-7 (2024)

Abstract In the present work, we report the development of a rapid, efficient, and solvent-free procedure for the N-methylation of secondary amines under mechanochemical conditions. After optimization of the milling parameters, a vibrational ball mil

Externí odkaz: https://doaj.org/article/f7f71ec5fb1845edbcb2ac31681fb233

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Akademický článek

Development of potent and effective SARS-CoV-2 main protease inhibitors based on maleimide analogs for the potential treatment of COVID-19

Autor: Karol Biernacki, Olga Ciupak, Mateusz Daśko, Janusz Rachon, Damian Flis, Justyna Budka, Iwona Inkielewicz-Stępniak, Anna Czaja, Janusz Rak, Sebastian Demkowicz

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 39, Iss 1 (2024)

AbstractIn the present work, we report a new series of potent SARS-CoV-2 Main Protease (Mpro) inhibitors based on maleimide derivatives. The inhibitory activities were tested in an enzymatic assay using recombinant Mpro (3CL Protease from coronavirus

Externí odkaz: https://doaj.org/article/cdb6c235654144bfbb03ab8413a8952f

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Akademický článek

Design, synthesis and biological evaluation of novel N-phosphorylated and O-phosphorylated tacrine derivatives as potential drugs against Alzheimer’s disease

Autor: Maja Przybyłowska, Krystyna Dzierzbicka, Szymon Kowalski, Sebastian Demkowicz, Mateusz Daśko, Iwona Inkielewicz-Stepniak

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 37, Iss 1, Pp 1012-1022 (2022)

In this work, we designed, synthesised and biologically investigated a novel series of 14 N- and O-phosphorylated tacrine derivatives as potential anti-Alzheimer’s disease agents. In the reaction of 9-chlorotacrine and corresponding diamines/aminoa

Externí odkaz: https://doaj.org/article/58e48df46aaa456083f2bc23928b953c

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Akademický článek

New potent steroid sulphatase inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives

Autor: Olga Ciupak, Mateusz Daśko, Karol Biernacki, Janusz Rachon, Maciej Masłyk, Konrad Kubiński, Aleksandra Martyna, Sebastian Demkowicz

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 36, Iss 1, Pp 239-248 (2021)

In the present work, we report a new class of potent steroid sulphatase (STS) inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives. Within the set of new STS inhibitors, 6-(1-(1,2,3-trifluorophenyl)-1H-1,2,3-tr

Externí odkaz: https://doaj.org/article/1d8fdeadde00449b96ff653055b93fa6

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Akademický článek

Recent progress in the development of steroid sulphatase inhibitors – examples of the novel and most promising compounds from the last decade

Autor: Mateusz Daśko, Sebastian Demkowicz, Karol Biernacki, Olga Ciupak, Witold Kozak, Maciej Masłyk, Janusz Rachon

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 35, Iss 1, Pp 1163-1184 (2020)

The purpose of this review article is to provide an overview of recent achievements in the synthesis of novel steroid sulphatase (STS) inhibitors. STS is a crucial enzyme in the biosynthesis of active hormones (including oestrogens and androgens) and

Externí odkaz: https://doaj.org/article/f089a2247d0c42ee9b6e9c28a518045c

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Akademický článek

Novel 1,2,3-Triazole Derivatives as Mimics of Steroidal System—Synthesis, Crystal Structures Determination, Hirshfeld Surfaces Analysis and Molecular Docking

Autor: Mateusz Daśko, Anna Dołęga, Magdalena Siedzielnik, Karol Biernacki, Olga Ciupak, Janusz Rachon, Sebastian Demkowicz

Publikováno v: Molecules, Vol 26, Iss 13, p 4059 (2021)

Herein, we present the synthesis and crystal structures determination of five 4-(1-phenyl-1H-1,2,3-triazol-4-yl)phenol derivatives containing halogen atoms, 6a–e, which may be used as an excellent mimic of steroids in the drug development process.

Externí odkaz: https://doaj.org/article/aed464f0ec7e4020bc5648ce1c254479

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Akademický článek

Novel 1,2,4-Oxadiazole Derivatives in Drug Discovery

Autor: Karol Biernacki, Mateusz Daśko, Olga Ciupak, Konrad Kubiński, Janusz Rachon, Sebastian Demkowicz

Publikováno v: Pharmaceuticals, Vol 13, Iss 6, p 111 (2020)

Five-membered 1,2,4-oxadiazole heterocyclic ring has received considerable attention because of its unique bioisosteric properties and an unusually wide spectrum of biological activities. Thus, it is a perfect framework for the novel drug development

Externí odkaz: https://doaj.org/article/9781be4164914d6fbd2c951d3f7f303d

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