Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Janusz Rachoń"'
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
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
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
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
Publikováno v:
Journal of Inclusion Phenomena & Macrocyclic Chemistry; Aug2008, Vol. 61 Issue 3/4, p381-391, 11p
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
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
Publikováno v:
Liebigs Annalen der Chemie. 1981:709-718
Isocyanmethylphosphonsaure-diethylester (3) laβt sich baseninduziert (Kalium-tert-butylat oder Natriumhydrid in Methylendichlorid) zu hoheren 1-Isocyanalkylphosphonsaure-diethylestern 5 mono- oder dialkylieren. Diese ergeben bei der sauren Hydrolyse
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::cf2a32186afc4ad23ac5755d32e384a5
https://doi.org/10.1002/jlac.198119810417
https://doi.org/10.1002/jlac.198119810417
Publikováno v:
Liebigs Annalen der Chemie. 1981:1693-1698
(Isocyanmethyl)phosphonsaure-diethylester (5a) liefert nach Metallieren mit Kalium-tert-butylat mit Chlorameisensaureestern oder Carbamoylchloriden (Typ 6) bzw. mit Methylisocyanat (10) die 4-Oxazolylphosphonsaure-diethylester 9 mit einer maskierten
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ca1f4cc0c3329c5dacb21002f5392b4c
https://doi.org/10.1002/jlac.198119810918
https://doi.org/10.1002/jlac.198119810918
Autor:
Ulrich Schöllkopf, Janusz Rachoń
Publikováno v:
Liebigs Annalen der Chemie. 1981:1186-1189
Aus α-metalliertem Isocyanmethylphosphonsaure-diethylester (1) erhielt man mit Acylchloriden oder -imidazoliden (Typ 3) die Oxazol-4-ylphosphonsaure-diethylester 7, mit Schwefelkohlenstoff gefolgt von Methyliodid-Addition (5-Methylthiothiazol-4-yl)p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::87c99157baca4953be6bdcf250b3c58b
https://doi.org/10.1002/jlac.198119810704
https://doi.org/10.1002/jlac.198119810704