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Flavonoids as inhibitors of human neutrophil elastase
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Clays as Inhibitors of Polyurethane Foams’ Flammability
PublicationPolyurethanes are a very important group of polymers with an extensive range of applications in different branches of industry. In the form of foams, they are mainly used in bedding, furniture, building, construction, and automotive sectors. Due to human safety reasons, these applications require an appropriate level of flame retardance, often required by various law regulations. Nevertheless, without the proper modifications,...
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Mrówczan sodu z nowym pakietem inhibitorów korozji jako ekologiczny środek do odladzania infrastruktury lotniczej.
PublicationPrzedstawiono wyniki badań korozji kadmowej powłoki na stali oraz korozji po zanurzeniu stopów metali w mrówczanie sodu z nowym pakietem inhibitorów korozji, zawierającym synergiczną kompozycję poliasparaginianu sodu oraz imidazolu. Ponadto wyznaczono zdolność penetracji lodu przez badany układ. Właściwo- ści opracowanej kompozycji odladzającej porównano z właściwościami środków dostępnych na rynku. Uzyskane wyniki wskazują, że otrzymany...
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COMPUTER-AIDED DESIGN OF ORGANOPHOSPHORUS INHIBITORS OF UREASE
PublicationBased on the structure of the most potential inhibitor diamidophosphate, various novel groups of inhibitors were developed by knowledge-based design approach with covalent carbon-phosphorus or carbon-phosphorus-carbon bond to improve hydrolytic stability to inhibit the microbial ureases. Designed compounds were evaluated with 10 (LigScore1, LigScore2, PLP1, PLP2, JAIN, PMF, PMF04, LUDI_1, LUDI_2 and LUDI_3) different scoring functions...
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Synthesis of anthraquinone-tuftsin analogues as potential topoisomerase inhibitors
PublicationZaprezentowano syntezę nowych analogów antrachinonów z pochodnymi tuftsyny i retro-tuftsyny oraz wstępne badania biologiczne (aktywność cytotoksyczną na wybranych liniach nowotworowych oraz zdolność hamowania topoizomerazy I).
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Pochodne fosforylowanych cukrów jako inhibitory syntazy glcn-6-p
PublicationW artykule został opisany mechanizm działania syntazy glukozamino-6-fosforanu i syntezy wybranych analogów blokujących domenę wiążących D-fruktozo-6-fosforanu, którym jest cis-enolamina.
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Substrate specificity and inhibitory study of human airway trypsin-like protease
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Synthesis and Cholinesterase Inhibitory Activity of N-Phosphorylated /N-Tiophosphorylated Tacrine
PublicationNovel phosphorus and thiophosphorus tacrine derivatives were designed, synthesized and their biological activity and molecular modeling was investigated as a new potential anti-Alzheimer's disease (AD) agents. All new synthesized compound exhibited lower toxicity against neuroblastoma cell line (SH-SY5Y) in comparison with tacrine. Two analogues in the series, 7 and 9, demonstrated lack of cytotoxicity against hepatocellular cells...
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Nowe estrowe i amidowe pochodne inhibitorów syntazy glukozamino-6-fosforanu - synteza i aktywność biologiczna
PublicationPrzedmiotem rozprawy doktorskiej są modyfikacje chemiczne analogów glutaminy – kwasu N3-(4-metoksyfumaroilo)-S-2,3-diaminopropanowego (FMDP) oraz kwasu N3-[(E)-4-fenylo-4-okso-2-butenoilo]-S-2,3-diaminoaminopropanowego (BADP). Związki te są inhibitorami syntazy glukozamino-6-fosforanu i mimo ich silnych właściwości inhibicyjnych, nie wykazują zdolności do hamowania wzrostu drobnoustrojów. Brak aktywności przeciwdrobnoustrojowej...
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New potent cathepsin G phosphonate inhibitors
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ACEI and ARB — Each Unique RAAS Inhibitors
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HDAC Inhibitors: Innovative Strategies for Their Design and Applications
PublicationHistone deacetylases (HDACs) are a large family of epigenetic metalloenzymes that are involved in gene transcription and regulation, cell proliferation, differentiation, migration, and death, as well as angiogenesis. Particularly, disorders of the HDACs expression are linked to the development of many types of cancer and neurodegenerative diseases, making them interesting molecular targets for the design of new efficient drugs...
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Therapeutic Potential of Multifunctional Derivatives of Cholinesterase Inhibitors
PublicationThe aim of this work is review of tacrine analogues from the last three years, which were not included in the latest review work, donepezil and galantamine hybrids from 2015 and rivastigmine derivatives from 2014. In this account we summarize the efforts toward the development and characterization of non-toxic inhibitors of cholinesterases based on mentioned drugs with various interesting additional properties such as antioxidant,...
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Inhibitors of amino acids biosynthesis as antifungal agents
PublicationFungal microorganisms, including the human pathogenic yeast and filamentous fungi, are able to synthesize all proteinogenic amino acids, including nine that are essential for humans. A number of enzymes catalyzing particular steps of human-essential amino acid biosynthesis are fungi specific. Numerous studies have shown that auxotrophic mutants of human pathogenic fungi impaired in biosynthesis of particular amino acids exhibit...
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Catalytic topoisomerase II inhibitors in cancer therapy.
PublicationDNA topoizomeraza II jest jednym z głównych celów molekularnych dla leków stosowanych w terapii przeciwnowotworowej. Wszystkie inhibitory tego enzymu są zdolne do zakłócania w jeden z etapów cyklu katalitycznego topoizomerazy II. Związki, które stabilizują kowalencyjny kompleks DNa i topoizomerazy II (znany jako kompleks rozszczepialny) są nazywane truciznami topoizomerazy, inne związki, które hamują aktywność enzymu na innych...
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In vitro enzyme inhibitory properties, antioxidant activities, and phytochemical profile of Potentilla thuringiaca
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Synthesis and antimicrobial and nitric oxide synthase inhibitory activities of novel isothiourea derivatives
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Synthesis and steroid sulfatase inhibitory activities of N-alkanoyl tyramine phosphates and thiophosphates
PublicationA series of phosphate and thiophosphate analogs based on the frameworks of N-alkanoyl tyramines have been synthesized and biologically evaluated. Their binding modes have been modeled using docking techniques. The inhibitory effects of the synthesized compounds were tested on STS isolated from the human placenta as well as the MCF-7, MDA-MB-231 and SkBr3 cancer cell lines. Most of the new STS inhibitors possessed potent activity...
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Metodyka rozdzielania i oznaczania lotnych inhibitorów fermentacji w brzeczkach fermentacyjnych ciemnej fermentacji, techniką GC-MS
PublicationW pracy przedstawiono opracowaną w wyniku badań metodykę identyfikacji i oznaczania inhibitorów fermentacji w brzeczkach fermentacji ciemnej z biomasy ligno-celulozowej, z wykorzystaniem ekstrakcji ciecz-ciecz w sprzężeniu z chromatografią gazową ze spektrometrem mas (LLE-GC-MS). W ramach badań dokonano doboru korzystnych warunków ekstrakcji ciecz-ciecz, w tym: pH, objętości rozpuszczalnika ekstrakcyjnego, czasu ekstrakcji oraz warunków...
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Enhanced sorption of inhibitory compounds from fermentation broth using a MOF@pseudo-DES composite
PublicationThe increase in biorefinery processes underscores the need for effective biofuel generation; nevertheless, inhibitors such as hydroquinone (HQ), 5-hydroxymethylfurfural (HMF), furfural (FF), and vanillin (VAN) resulting from biomass degradation impede microbial growth and process efficiency. Herein, a deep eutectic solvent (DES)-like substance was in-situ generated on the surface of NH2-UiO-66 via a post-synthetic coating process...
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An Overview of Several Inhibitors for Alzheimer’s Disease: Characterization and Failure
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Synthesis of the inosine 5′-monophosphate dehydrogenase (IMPDH) inhibitors
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CDK9 inhibitors in multiple myeloma: a review of progress and perspectives
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Low-Molecular-Weight Aldehyde Inhibitors of Cathepsin G
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Inhibitors of cathepsin G: a patent review (2005 to present)
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Direct renin inhibitors in hypertension – Approaching the moment of truth
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Cyclic Peptidic Furin Inhibitors Developed by Combinatorial Chemistry
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Phosphate and Thiophosphate Biphenyl Analogs as Steroid Sulfatase Inhibitors
PublicationIn the present work, we report convenient methods for the synthesis and biological evaluation of phosphate and thiophosphate biphenyl derivatives exhibiting steroid sulfatase (STS) activity. The described synthesis is based on straightforward preparation of biphenyl-4-ol and 40-hydroxybiphenyl- 4-carboxylic acid ethyl ester modified with various phosphate or thiophosphate moieties. The inhibitory effects of these compounds were...
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Synthesis of bicoumarin thiophosphate derivatives as steroid sulfatase inhibitors
PublicationBased on the frameworks of 7-hydroxy-2,3-dihydro-1H-cyclopenta[c]chromen-4-one, 3-hydroxy- 7,8,9,10-tetrahydro-6H-benzo[c]chromen-6-one and 3-hydroxy-8,9,10,11-tetrahydro-7H-cyclohepta[c] chromen-6-one, a series of bicoumarin thiophosphate analogs have been synthesized and biologically evaluated. Additionally, their binding modes have been modeled using docking techniques. The inhibitory properties of the synthesized compounds...
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Inhibitors of angiogenesis in cancer therapy – synthesis and biological activity
PublicationAngiogenesis is the process of formation of new capillaries from preexisting blood vessels. Angiogenesis is involved in normal physiological processes, and plays an important role in tumor invasion and development of metastases. Vascular endothelial growth factor (VEGF) plays a key role in angiogenesis. VEGF is a mitogen for vascular endothelial cells and stimulates their proliferation. By inhibiting the biological activity of...
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Synthesis of the inosine 5'-monophosphate dehydrogenase (IMPDH) inhibitors
PublicationIn this review are summrized newly described IMPDH inhibitors. The article concerns both synthetic pathways and biological activities of the most promising compounds.
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Variability of Hordeum vulgare L. Cultivars in Yield, Antioxidant Potential, and Cholinesterase Inhibitory Activity
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Procognitive activity of nitric oxide inhibitors and donors in animal models
PublicationNitric oxide is a small gaseous molecule that plays important roles in the majority of biological functions. Impairments of NO-related pathways contribute to the majority of neurological disorders, such as Alzheimer’s disease (AD), and mental disorders, such as schizophrenia. Cognitive decline is one of the most serious impairments accompanying both AD and schizophrenia. In the present study, the activities of NO donors, slow (spermine...
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Carboxylic acids as efficient corrosion inhibitors of aluminium alloys in alkaline media
PublicationThe efficiency of AA5754 aluminium alloy corrosion inhibition achieved with maleic, malic, succinic, tartaric, citric, tricarballylic acids and serine in alkaline environment (pH 11) was examined. Selected corrosion inhibitors are characterized by different numbers and distribution of carbonyl and hydroxyl groups within their molecules. We have proposed and verified a novel approach for determining the adsorption isotherms based...
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Synthesis of novel, peptidic kinase inhibitors with cytostatic/cytotoxic activity
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Steroid Sulfatase Inhibitors Based on Phosphate and Thiophosphate Flavone Analogs
PublicationA series of phosphate and thiophosphate flavone derivatives were synthesized and biologically evaluated in vitro for inhibition of steroid sulfatase (STS) activity. The described synthesis includes the straightforward preparation of 7-hydroxy-2-phenyl-4H-chromen-4-one 3a, 2-(4-fluorophenyl)-7-hydroxy-4H-chromen-4-one 3b, 7-hydroxy-2-(4-(trifluoromethyl)phenyl)-4H-chromen-4-one 3c, 7-hydroxy-2-(p-tolyl)-4H-chromen-4-one 3d modified...
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Inhibitors of glucosamine-6-phosphate synthase as potential antifungal drugs.
PublicationPrzedstawiono stan obecny i perspektywy zastosowania inhibitorów enzymu syntazy GlcN-6-P jako leków skutecznych w leczeniu grzybic układowych. Używając metod modelowania molekularnego zaprojektowano struktury inhibitorów enzymu należących do dwóch grup strukturalnych: analogów glutaminy oraz analogów stanu przejściowego reakcji katalizowanej przez enzym. Opracowano metody syntezy pochodnych zoptymalizowanych inhibitorów, wykazujących...
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Both activating and inhibitory Fc gamma receptors mediate rituximab-induced trogocytosis of CD20 in mice
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ACE Inhibitory Properties and Phenolics Profile of Fermented Flours and of Baked and Digested Biscuits from Buckwheat
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Inhibitory and antimicrobial activities of OGTI and HV-BBI peptides, fragments and analogs derived from amphibian skin
PublicationA series of linear and cyclic fragments and analogs of two peptides (OGTI and HV-BBI) isolated from skin secretions of frogs were synthesized by the solid-phase method. Their inhibitory activity against several serine proteinases: bovine beta-trypsin, bovine alpha-chymotypsin, human leukocyte elastase and cathepsin G from human neutrophils, was investigated together with evaluation of their antimicrobial activities against Gram-negative...
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Metodyka oznaczania sumarycznej zawartości inhibitorów fermentacji ciemnej oraz monocukrów w brzeczkach fermentacyjnych techniką HPLC-RID-UV-VIS/DAD
PublicationW pracy przedstawiono wyniki badań oraz opracowaną w ich rezultacie metodykę ilościowego oznaczania sumarycznej zawartości inhibitorów fermentacji ciemnej oraz monocukrów w brzeczkach fermentacyjnych z wykorzystaniem techniki chromatografii cieczowej (RP-HPLC-RID-UV-VIS/DAD). Najbardziej przydatną do zbadania sumarycznej zawartości inhibitorów w próbkach rzeczywistych okazało się zastosowanie warunków chromatografii wykluczania...
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Projektowanie, synteza oraz badanie aktywności biologicznej nowych inhibitorów sulfatazy steroidowej (STS) na bazie amidosiarczanowych pochodnych triazoli i oksadiazoli
PublicationNiniejsza dysertacja dotyczy szeregu badań z wykorzystaniem technik modelowania molekularnego oraz metod syntezy nowych inhibitorów STS opartych o rdzenie pierścieni heterocyklicznych 1,2,3-triazolu oraz 1,2,4-oksadiazolu. Aktywność inhibicyjna otrzymanych pochodnych została oznaczona w testach in vitro z wykorzystaniem enzymu wyizolowanym z łożyska ludzkiego oraz znakowanym radioizotopowo siarczanem estronu, a także w teście komórkowych...
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Chocolate desserts with ricotta hydrolysates: In vitro study of inhibitory activity against angiotensin‐converting enzyme and cholinesterase
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Influence of sub-inhibitory concentration of selected plant essential oils on the physical and biochemical properties of Pseudomonas orientalis
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Antiplasmodial Activity of Nitroaromatic Compounds: Correlation with Their Reduction Potential and Inhibitory Action on Plasmodium falciparum Glutathione Reductase
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Inhibitory Effect of Eugenol and trans‐Anethole Alone and in Combination with Antifungal Medicines on Candida albicans Clinical Isolates
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N-Alkyl Derivatives of L-Glutamine As Inhibitors of Glutamine - Utilizing Enzymes
PublicationA general facile method to synthesize the N-gamma-alkyl and N-gamma,N-gamma-dialkyl derivatives of L-glutamine (1a-d) from L-glutamic acid as a starting substrate is presented. The obtained compounds are shown to inhibit three diferent glutamine-utilizing enzymes, namely: glutaminase, gamma-glutamyl transpeptidase, and glucosamine-6-phosphate synthase, with inhibitory constants within the milimolar range.
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Acetylcholinesterase inhibitors: structure-activity relationship and kinetic studies on selected flavonoids
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The Combination of Beta-Blockers and ACE Inhibitors Across the Spectrum of Cardiovascular Diseases
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Computational Selectivity Assessment of Protease Inhibitors against SARS-CoV-2
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