NEWS

Dr. Paweł Borowiecki became an Affiliate member of the Royal Society of Chemistry

We want to inform you that Dr. Borowiecki has been invited to join the elite group of Affiliate Members of the Royal Society of Chemistry. It is worth mentioning that the favorable decision was determined by the high scientific level of articles published this year in prestigious journals of the Royal Society of Chemistry. We invite all interested persons to read those publications at Catalysis Science & Technology and RSC Advances

(date: 11.08.2022)

LBB-WUT crew published a new paper in RSC Advances

We are delighted to announce that the publication entitled: Development of a novel chemoenzymatic route to enantiomerically enriched β-adrenolytic agents. A case study toward propranolol, alprenolol, pindolol, carazolol, moprolol, and metoprolol” has been published in RSC Advances (ISSN: 2046-2069, IF: 4.036).

This article reports on efficient chemoenzymatic routes toward both enantiomers of β-blockers, which were accomplished by identifying a central chiral building block prepared using either lipase-catalyzed kinetic resolution methodology or ADH-catalyzed biotranshydrogenation. This work is another excellent example of fruitful collaboration of our lab team with Prof. Wolfgang Kroutil from the University of Graz.

P.S. We are happy to say ufffff …. we made it! It was as hard as establishing a new route in the high mountains!

These studies were funded by the National Science Center (NCN) of Poland grant „SONATA 15” (Grant No. 2019/35/D/ST4/01556).

(date: 10.08.2022)

LBB-WUT crew published a new paper in Bioorganic Chemistry

We are pleased to announce that the publication entitled: „Biocatalytic Hydrogen-Transfer To Access Enantiomerically Pure Proxyphylline, Xanthinol, and Diprophylline” has been published in Bioorganic Chemistry (ISSN: 0045-2068, IF: 5.307).

This article reports on a novel biocatalytic synthetic route toward optically pure xanthine-based APIs, which are very useful as efficient bronchial vasodilators. It is worth noting that this work was carried out in international cooperation with Professor Wolfgang Kroutil from the University of Graz, Austria (Karl-Franzens-Universität Graz). We also want to inform you that this article has been dedicated in memory of Prof. Jacek K. Gawroński (1943–2020), who was a fabulous scientist, academic tutor, and author of the cult academic textbook entitled: „Stereochemistry in Organic Synthesis”!

These studies were funded by the National Science Center (NCN) of Poland grant „SONATA 15” (Grant No. 2019/35/D/ST4/01556).

(date: 14.06.2022)

LBB-WUT crew published a new paper in Catalysis Science & Technology

We are delighted to announce that the publication entitled: „Chemoenzymatic deracemization of lisofylline catalyzed by a (laccase/TEMPO)-alcohol dehydrogenase system” has been published in Catalysis Science & Technology (ISSN: 2044-4761, IF: 6.177).

This article reports on a novel biocatalytic method for the synthesis of both enantiomers of lisofylline based on Trametes versicolor laccase, TEMPO as a redox mediator, and stereocomplementary recombinant alcohol dehydrogenases as biocatalysts. It is also worth noting that this work was carried out in international cooperation with Professor Wolfgang Kroutil from the University of Graz, Austria (Karl-Franzens-Universität Graz). By the way, we are pleased that this paper is our first one accepted in the journal published by the Royal Chemical Society (RSC), and we hope not the last! This is also a first paper published by our first-year PhD Student – Ola Rudzka. Congrads for her!

These studies were funded by the National Science Center (NCN) of Poland grant „SONATA 15” (Grant No. 2019/35/D/ST4/01556).

(date: 16.05.2022)

LBB-WUT crew published a new paper in Catalysts

We are pleased to announce that the publication entitled: „Expanding Access to Optically Active Non-Steroidal Anti-Inflammatory Drugs via Lipase-Catalyzed KR of Racemic Acids Using Trialkyl Orthoesters as Irreversible Alkoxy Group Donors” has been published in Catalysts (ISSN: 2073-4344, IF: 4.501) and is a part of Special Issue „Applications of Hydrolases in Medicinal Chemistry” hosted by Dr. Borowiecki and Dr. Koszelewski from IChO PAS.

This article reports on a novel biocatalytic method for the synthesis of enantiomerically enriched blockbuster (S)-profens, namely naproxen, ibuprofen, flurbiprofen, and ketoprofen. It is also worth noting that this work was carried out in cooperation with Dr. Jan Kutner from the Laboratory for Structural and Biochemical Research, Biological and Chemical Research Centre, Department of Chemistry, University of Warsaw. 

These studies were funded by the National Science Center (NCN) of Poland grant „SONATA 15” (Grant No. 2019/35/D/ST4/01556).

(date: 16.05.2022)

Dr. Paweł Borowiecki’s publication on the cover of ACS Sustainable Chemistry & Engineering

We are delighted to share our research published in ACS Sustainable Chemistry & Engineering (IF = 8.198) demonstrating an innovative and cost-effective lipase-catalyzed kinetic resolution of secondary alcohols based on a fully renewable and non-toxic α-angelica lactone as an irreversible acylating agent. The designed biocatalytic approach was integrated with a simple Girard’s P reagent strategy, which can be performed on a multi-gram scale, leading to enantiomerically pure pharmaceutically relevant building blocks isolated in satisfactory yields without using preparative chromatography. Furthermore, the elaborated methodology based on extractive purification strategy reduces the emission of volatile solvents, eliminates hazardous materials, such as cancerogenic silica gel and vinyl acetate, and enables more process waste to be recycled. Therefore, it might open avenues for possible broader synthetic applications in the resolution of enantiomers useful in the pharamceuticals manufacturing. We hope that over two years of research in a narrow collaboration between Dr. Borowiecki and Dr. Poterała from the Chair of Organic Chemistry WUT resulted in an impactful manuscript. The paper is entitled: „From Waste to Value – Direct Utilization of α-Angelica Lactone as a Non-conventional Irreversible Acylating Agent in a Chromatography-free Lipase-catalyzed KR Approach Towards sec-Alcohols” and was also recognized by the Journal’s Editors as 'a very important paper’ by highlighting it with the Cover art work.

                                           

These studies were funded by the National Science Center (NCN) of Poland grant „SONATA 15” (Grant No. 2019/35/D/ST4/01556).

(date: 07.08.2021)

NEW paper of our Lab-Team in the International Journal of Molecular Sciences

We are pleased to announce that the publication of Dr Borowiecki, entitled: ‘Synthesis of Novel Acyl Derivatives of 3‐(4,5,6,7‐Tetrabromo‐1H‐benzimidazol‐1‐yl)propan‐1‐ols — Intracellular TBBi‐Based CK2 Inhibitors with Proapoptotic Properties’ was published in highly prestigious International Journal of Molecular Sciences (ISSN: 1422-0067, IF: 5.923).

It is worth noting that this research was carried out in cooperation with scientists from the National Institute of Medicines and the Nencki Institute of Experimental Biology of the Polish Academy of Sciences and raises important aspects concerning the synthesis of polybrominated benzoazole prodrugs and their inhibitory activity toward CK2 protein kinase as well as anti-cancer properties against breast cancer cells. The article was published in the Open Access (OA) model, which greatly increases the chances of its wider impact.

(date: 10.06.2021)

LBB-WUT crew published a new paper in Frontiers in Chemistry

We are pleased to announce that the publication entitled: ’The First Insight Into the Supramolecular System of D,L-α-Difluoromethylornithine: A New Antiviral Perspective’ has been published in Frontiers in Chemistry (ISSN: 2296-2646, IF: 5.221).

It is worth noting that this work was carried out in international cooperation with researchers from the UK, Slovakia and Poland (Dr Joanna Bojarska and Prof. Wojciech Wolf) and reports on an important aspects of the molecular basis of biological activity of DFMO and its halogenated analogs. 

(date: 15.05.2021)

LBB-WUT crew with a new paper in Molecular Catalysis journal

We are extremely happy that our new paper on ‘Chemoenzymatic Enantioselective and Stereo-Convergent Syntheses of Lisofylline Enantiomers via Lipase-catalyzed Kinetic Resolution and Optical Inversion Approach’ was published today in Molecular Catalysis (ISSN: 2468-8231; IF: 5.062)!

We hope that our paper will help medicinal chemists to prepare this enantiomeric API in preparative scale to complete on-going clinical trials on extremely interesting pharmacological properties of its enantiomers. Congrats to all authors!

(date: 18.03.2021)

Dr Borowiecki & Dr Koszelewski as a Guest Editors for Special Issue “Applications of Hydrolases in Medicinal Chemistry

We are proud to announce that Doctor Borowiecki together with his colleague from IChO PAS, Dr Dominik Koszelewski, will coordinate the edition of a Special Issue of the journal Catalysts (ISSN 2073-4344; IF: 4.146), entitled: “Applications of Hydrolases in Medicinal Chemistry”. The aims of this Special Issue are as follows: the application of hydrolases for chemoenzymatic syntheses of new compounds of defined biological activities; development of novel or significantly-improved hydrolase-catalyzed routes toward key pharmaceutical intermediates and/or enantiomeric drugs; biotransformations carried out using isolated enzymes and/or whole-cell biocatalysts.

The deadline for collaboration is now open.

See: https://www.mdpi.com/journal/catalysts/special_issues/hydrolases_medicinal for details of the submission.

hydrolases_medicinal-flyer.pdf

(date: 01.03.2021)

LBB-WUT crew with a new paper in Bioorganic Chemistry journal

We are pleased to announce that a new article entitled: ‘Chemoenzymatic synthesis of enantiomerically enriched diprophylline and xanthinol nicotinate’ from the members of LBB-WUT is available in the Bioorganic Chemistry (ISSN: 0045-2068; IF: 5.275). We hope that this paper will inspire other researchers to elaborate alternative asymmetric routes toward optically active broncho- and vaso-dilators.

More info on this topic can be found: https://www.sciencedirect.com/science/article/abs/pii/S0045206820317466

(date: 01.02.2021)