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The Evaluation of DHPMs as Biotoxic Agents on Pathogen Bacterial Membranes 

Gawdzik, Barbara; Kowalczyk, Paweł; Koszelewski, Dominik; Brodzka, Anna; Masternak, Joanna; Kramkowski, Karol; Wypych, Aleksandra; Ostaszewski, Ryszard (MDPI, 2022)
Herein, we present biological studies on 3,4-dihydropyrimidin-2(1H)-ones (DHPMs) obtained via Biginelli reaction catalyzed by NH4Cl under solvent-free conditions. Until now, DHPMs have not been tested for biological activity ...
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Computer-designed repurposing of chemical wastes into drugs 

Wołos, Agnieszka; Koszelewski, Dominik; Roszak, Rafał; Szymkuć, Sara; Moskal, Martyna; Ostaszewski, Ryszard; Brezicki, Gordon; Samuel, Jonathon; McQuade, D. Tyler; Rogers, Luke; Grzybowski, Bartosz A.; Herrera, Brenden T.; Maier, Josef M.; Lummiss, Justin A. M. (Nature, 2022-04-27)
As the chemical industry continues to produce considerable quantities of waste chemicals1,2, it is essential to devise ‘circular chemistry’3,4,5,6,7,8 schemes to productively back-convert at least a portion of these unwanted ...
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Simultaneous Enantiodivergent Synthesis of Diverse Lactones and Lactams via Sequential One-Pot Enzymatic Kinetic Resolution–Ring-Closing Metathesis Reactions 

Brodzka, Anna; Koszelewski, Dominik; Ostaszewski, Ryszard (MDPI, 2022)
One of the goals of diversity-oriented synthesis is to achieve the structural diversity of obtained compounds. As most biologically active compounds are chiral, it is important to develop enantioselective methods of their ...
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Intensification of Double Kinetic Resolution of Chiral Amines and Alcohols via Chemoselective Formation of a Carbonate–Enzyme Intermediate 

Samsonowicz-Górski, Jan; Brodzka, Anna; Ostaszewski, Ryszard; Koszelewski, Dominik (MDPI, 2022)
Chiral amines and alcohols are synthons of numerous pharmaceutically-relevant compounds. The previously developed enzymatic kinetic resolution approaches utilize a chiral racemic molecule and achiral acyl donor (or acyl ...
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Influence of Open Chain and Cyclic Structure of Peptidomimetics on Antibacterial Activity in E. coli Strains 

Sahrawat, Parul; Kowalczyk, Paweł; Koszelewski, Dominik; Szymczak, Mateusz; Kramkowski, Karol; Wypych, Aleksandra; Ostaszewski, Ryszard (MDPI, 2022)
An efficient method for the synthesis of functionalized peptidomimetics via multicomponent Ugi reaction has been developed. The application of trifluoroethanol (TFE) as a reaction medium provided desired products with good ...
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Synthesis and Antimicrobial Activity of the Pathogenic E. coli Strains of p-Quinols: Additive Effects of Copper-Catalyzed Addition of Aryl Boronic Acid to Benzoquinones 

Koszelewski, Dominik; Kowalczyk, Paweł; Samsonowicz-Górski, Jan; Hrunyk, Anastasiia; Brodzka, Anna; Łęcka, Justyna; Kramkowski, Karol; Ostaszewski, Ryszard (MDPI, 2023)
A mild and efficient protocol for the synthesis of p-quinols under aqueous conditions was developed. The pivotal role of additives in the copper-catalyzed addition of aryl boronic and heteroaryl boronic acids to benzoquinones ...
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Wheat germ lipase: isolation, purification and applications 

Kublicki, Marcin; Koszelewski, Dominik; Brodzka, Anna; Ostaszewski, Ryszard (Taylor and Francis, 2022)
In recent years, wheat germ lipase (WGL) is attracting considerable interest. To date, several WGL applications have already been described: (i) fats and oils modification; (ii) esterification reactions in organic media, ...
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Promiscuous Lipase-Catalyzed Knoevenagel–Phospha–Michael Reaction for the Synthesis of Antimicrobial β-Phosphono Malonates 

Samsonowicz-Górski, Jan; Koszelewski, Dominik; Kowalczyk, Paweł; Śmigielski, Paweł; Hrunyk, Anastasiia; Kramkowski, Karol; Wypych, Aleksandra; Szymczak, Mateusz; Lizut, Rafał; Ostaszewski, Ryszard (MDPI, 2022)
An enzymatic route for phosphorous–carbon bond formation was developed by discovering new promiscuous activity of lipase. We reported a new metal-free biocatalytic method for the synthesis of pharmacologically relevant ...
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Relationship between Structure and Antibacterial Activity of α-Aminophosphonate Derivatives Obtained via Lipase-Catalyzed Kabachnik−Fields Reaction 

Koszelewski, Dominik; Kowalczyk, Paweł; Śmigielski, Paweł; Samsonowicz-Górski, Jan; Kramkowski, Karol; Wypych, Aleksandra; Szymczak, Mateusz; Ostaszewski, Ryszard (MDPI, 2022)
We reported a new method dealing with the synthesis of novel pharmacologically relevant α-aminophosphonate derivatives via a lipase-catalyzed Kabachnik−Fields reaction with yields of up to 93%. The advantages of this ...
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Promiscuous Lipase-Catalyzed Markovnikov Addition of H-Phosphites to Vinyl Esters for the Synthesis of Cytotoxic α-Acyloxy Phosphonate Derivatives 

Kowalczyk, Paweł; Koszelewski, Dominik; Gawdzik, Barbara; Samsonowicz-Górski, Jan; Kramkowski, Karol; Wypych, Aleksandra; Lizut, Rafał; Ostaszewski, Ryszard (MDPI, 2022-03-07)
An enzymatic route for phosphorous-carbon- bond formation is developed by discovering new promiscuous activity of lipase. This biocatalytic transformation of phosphorous-carbon- bond addition leads to biologically and ...
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Koszelewski, Dominik (11)
Ostaszewski, Ryszard (11)Kowalczyk, Paweł (7)Kramkowski, Karol (7)Brodzka, Anna (6)... View MoreAffiliationInstitute of Organic Chemistry, Polish Academy of Sciences (9)Department of Physical Chemistry, Medical University of Bialystok (7)Department of Animal Nutrition, The Kielanowski Institute of Animal Physiology and Nutrition, Polish Academy of Sciences (6)... View MoreSubjectantimicrobial activity (5)lipopolysaccharide (LPS) (3)chemoselectivity (2)E. coli cells (2)enzyme promiscuity (2)... View MoreDate Issued2022 (10)2023 (1)LicenseCreative Commons Uznanie autorstwa 4.0 (10)Dozwolony użytek (1)

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