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Wyniki wyszukiwania dla: VETERINARY MEDICINE
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Immunosuppressive properties of amino acid and peptide derivatives of mycophenolic acid
PublikacjaMycophenolic acid (MPA) was coupled with amino acids and biologically active peptides including derivatives of tuftsin to modify its immunosuppressive properties. Both amino acid unit in the case of simple MPA amides and modifications within peptide moiety of MPA - tuftsin conjugates influenced the observed activity. Antiproliferative potential of the obtained conjugates was investigated in vitro and MPA amides with threonine methyl...
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Design, synthesis and high antitumor potential of new unsymmetrical bisacridine derivatives towards human solid tumors, specifically pancreatic cancers and their unique ability to stabilize DNA G-quadruplexes
PublikacjaNew promising unsymmetrical bisacridine derivatives (UAs), have been developed. Three groupsincluding 36 compounds were synthesized by the condensation of 4-nitro or 4-methylacridinone, imi-dazoacridinone and triazoloacridinone derivatives with 1-nitroacridine compounds linked with anaminoalkyl chain. Cytotoxicity screening revealed the high potency of these compounds against severaltumor cell lines. Particularly, imidazoacridinone-1-nitroacridine...
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A new 1-nitro-9-aminoacridine derivative targeting yeast topoisomerase II able to overcome fluconazole-resistance
PublikacjaFungal resistance remains a significant threat and a leading cause of death worldwide. Thus, overcoming microbial infections have again become a serious clinical problem. Although acridine derivatives are widely analyzed as anticancer agents, only a few reports have demonstrated their antifungal activity. In an effort to develop biologically active antifungals, twelve novel C-857 (9-(2′ -hydroxyethylamino)-1-nitroacridine) and...
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Fatty acids as molecular carriers in cleavable antifungal conjugates
PublikacjaConjugates composed of C2-18 fatty acid (FA) residues as a molecular carrier and 5-fluorocytosine (5-FC) as an active agent, released upon the action of intracellular esterases on the ester bond between FA and “trimethyl lock” intramolecular linker, demonstrate good in vitro activity against human pathogenic yeasts of Candida spp. The minimal inhibitory concentrations (MIC) values for the most active conjugates containing caprylic...
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Study of the anticancer potential of Cd complexes of selenazoyl-hydrazones and their sulfur isosters
PublikacjaThe biological activity of Cd compounds has been investigated scarce since Cd has been recognized as a human carcinogen. However, the toxicity of cadmium is comparable to the toxicity of noble metals such as Pt and Pd. The paradigm of metal toxicity has been challenged suggesting that metal toxicity is not a constant property, yet it depends on many factors like the presence of appropriate ligands. Studies on anticancer activity...
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From tryptophan to novel mitochondria-disruptive agent, synthesis and biological evaluation of 1,2,3,6-tetrasubstituted carbazoles
PublikacjaMitochondrial targeting plays an important role in anticancer therapy. The Mn(III)-promoted cyclization of 5- (1H-indol-3-yl)-3-oxopentanoic acid allow to obtain novel substituted carbazole derivatives that can act as mitochondria-disruptive agents. The starting materials used for the synthesis of these new aminocarbazoles are oxopentanoate derivatives of tryptophan. The scope and limitation of this method of synthesis are determined...
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Synthesis and biological activity of mycophenolic acid-amino acid derivatives
PublikacjaIn search of new immunosuppressants, mycophenolic acid (MPA) was coupled with amino acid methyl esters followed by hydrolysis to analogs bearing free carboxylic groups. The obtained compunds were tested in vitro as growth inhibitors of lymphoid cell line (Jurkat) and human peripheral blood mononuclear cells (PBMC) from healthy donors. According to obtained results recovering of free carboxylic group increased their activity. Additionally,...
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Carbonic anhydrase inhibitors. Synthesis, and molecular structure of novel series N-substituted N'-(2-arylmethylthio-4-chloro-5- methylbenzenesulfonyl)guanidines and their inhibition of human cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII
PublikacjaA series of novel N-substituted N'-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)guanidines 9 e41 have been synthesized and investigated as inhibitors of four isoforms of zinc enzyme carbonic anhydrase (CA.EC 4.2.1.1), that is the cytosolic CA I and II, and cancer-associated isozymes CA IX and XII. Against the human CA I investigated compounds showed KI in the range of 87e6506 nM, toward hCA II ranging from 7.8 to 4500 nM,...
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Structural factors affecting affinity of cytotoxic oxathiole-fused chalcones toward tubulin
PublikacjaSynthesis, in vitro cytotoxic activity, and interaction with tubulin of (E)-1-(6-alkoxybenzo[d][1,3]oxathiol- 5-yl)-3-phenylprop-2-en-1-one derivatives (2) are described. Some of the compounds demonstrated cytotoxic activity at submicromolar concentrations, and the activity could be related to interaction with tubulin at the colchicine binding site. Interaction of selected derivatives with tubulinwas evaluated using molecular modeling,...
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Synthesis and biological activity of novel ester derivatives of N3-(4-metoxyfumaroyl)-(S)-2,3-diaminopropanoic acid containing amide and keto function as inhibitors of glucosamine-6-phosphate synthase
PublikacjaA short series of novel ester derivatives of N3-4-methoxyfumaroyl-(S)-2,3-diaminopropanoic acid (FMDP) containing amido or keto functions have been designed and synthesized. Their antifungal activity and inhibitory properties toward fungal glucosamine-6-phosphate synthase has also been evaluated. The obtained compounds 11-13 and 15-17 demonstrated good antifunga activity against Candida albicans. Compounds 11-13 displayed also...
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Synthesis and antimicrobial activity of amino acid and peptide derivatives of mycophenolic acid
PublikacjaThe series of 16 novel amino acid and peptide mycophenolic acid (MPA) derivatives was obtained as potential antibacterial agents. Coupling of MPA with respective amines was optimized with condensing reagents such as EDCI/DMAP and T3P/TEA. Amino acid analogs were received both as methyl esters and also with the free carboxylic group. The biological activity of the products was tested on five references bacterial strains: Klebsiella...
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Novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(1,3,5-triazin-2-ylamino)guanidine derivatives: Inhibition of human carbonic anhydrase cytosolic isozymes I and II and the transmembrane tumor-associated isozymes IX and XII, anticancer activity, and molecular modeling studies
PublikacjaA series of novel 2-(2-arylmethylthio-4-chloro-5-methylbenzenesulfonyl)-1-(6-substituted-4-chloro-1,3,5-triazin-2-ylamino)guanidine derivatives 9–20 have been synthesized by substitution of chlorine atom at the 1,3,5-triazine ring in compounds 5–8 with 3- or 4-aminobenzenesulfonamide and 4-(aminomethyl)benzenesulfonamide hydrochloride. All the synthesized compounds were evaluated for their inhibitory activity toward hCA I, II,...
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Synthesis and antiproliferative activity of conjugates of adenosine with muramyl dipeptide and nor-muramyl dipeptide derivatives
PublikacjaWe synthesized a series of MDP(D,D) and nor-MDP(D,D) derivatives conjugated with adenosine through a spacer as potential immunosuppressants. New conjugates were evaluated on two leukemia cell lines (Jurkat and L1210) and PBMC from healthy donors.
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In vitro studies of antimicrobial activity of Gly-His-Lys conjugates as potential and promising candidates for therapeutics in skin and tissue infections
PublikacjaWe presented in vitro studies of antimicrobial activity of Gly-His-Lys conjugates that are important point in preliminary biological evaluation of their potential application in skin and tissue therapy. The novel compounds include the conjugation of fatty acids with a modification of the amino acid sequence in the primary structure of Gly-His-Lys.
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New Analogues of Mycophenolic Acid
PublikacjaMycophenolic acid (MPA) possesses antibacterial, antifungal, antiviral, immunosuppressive and anticancer properties. It is a non-competitive and reversible inhibitor of dehydrogenase inosine-5'-monophosphate (IMPDH). This compound belongs to the immunosuppressive drugs used for the prevention of both acute and chronic transplant rejection. Until now, two derivatives of MPA have been used clinically: mycophenolate mofetil (MMF,...
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Synthesis and biological evaluation of fluorinated N-benzoyl and N-phenylacetoyl derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as steroid sulfatase inhibitors
PublikacjaIn the present work, we report convenient methods for the synthesis of 3-(4-aminophenyl)-coumarin-7-O-sulfamate derivatives N-acylated with fluorinated analogues of benzoic or phenylacetic acid as steroid sulfatase (STS) inhibitors. The design of these potential STS inhibitors was supported by molecular modeling techniques. Additionally, computational docking methods were used to determine the binding modes of the synthesized inhibitors...
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Novel 2-(2-alkylthiobenzenesulfonyl)-3-(phenylprop-2-ynylideneamino)guanidine derivatives as potent anticancer agents – Synthesis, molecular structure, QSAR studies and metabolic stability
PublikacjaA series of new 2-(2-alkylthiobenzenesulfonyl)-3-(phenylprop-2-ynylideneamino)guanidine derivatives have been synthesized and evaluated in vitro by MTT assays for their antiproliferative activity against cell lines of colon cancer HCT-116, cervical cancer HeLa and breast cancer MCF-7. The obtained results indicated that these compounds display prominent cytotoxic effect. The best anticancer properties have been observed for derivatives...
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Synthesis and biological activity of novel mycophenolic acid conjugates containing nitro-acridine/acridone derivatives
PublikacjaOpracowano warunki reakcji kwasu mykofenolowego z aminowymi pochodnymi akrydyn i akrydonów. Tak otrzymane koniugaty zostały scharakteryzowane, a następnie przebadane in vitro pod względem aktywności przeciwbiałaczkowej oraz immunosupresyjnej.
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Synthesis, molecular structure, and metabolic stability of new series of N' -(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)-1-(5-phenyl-1 H -pyrazol-1-yl)amidine as potential anti-cancer agents
PublikacjaA series of new N'-(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)-1-(5-phenyl-1H-pyrazol-1-yl)amidine derivatives have been synthesized and evaluated in vitro by MTT assays for their antiproliferative activity against cell lines of colon cancer HCT-116, cervical cancer HeLa and breast cancer MCF-7. The studied compounds display selective activity mainly against HCT-116 and HeLa cells. Thus, five compounds show selective cytotoxic...
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Deep Learning-Based, Multiclass Approach to Cancer Classification on Liquid Biopsy Data
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Deep Learning-Based, Multiclass Approach to Cancer Classification on Liquid Biopsy Data
PublikacjaThe field of cancer diagnostics has been revolutionized by liquid biopsies, which offer a bridge between laboratory research and clinical settings. These tests are less invasive than traditional biopsies and more convenient than routine imaging methods. Liquid biopsies allow studying of tumor-derived markers in bodily fluids, enabling the development of more precise cancer diagnostic tests for screening, disease monitoring, and...
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PCR Melting Profile method for genotyping analysis of vancomycin-resistant Enterococcus faecium isolates from Hematological Unit patients
PublikacjaW ostatnich latach znacząco wzrasta liczba szczepów Enterococcus opornych na wankomycynę. Stwarzają one problemy medyczne u pacjentów skolonizowanych czy zainfekowanych tymi drobnoustrojami. W przedstawionych badaniach, określiliśmy genetyczne podobieństwo pomiędzy izolatami E. faecium VRE, pozyskiwanymi w okresie od kwietnia 2003 do kwietnia 2005 od pojedynczych pacjentów oddziału Hematologicznego Specjalistycznego Publicznego...
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Blok operacyjny
PublikacjaCentralnym punktem każdego współczesnego szpitala jest jego blok operacyjny. Rozwój technologii medycznej prowadzi do zmniejszenia roli hospitalizacji na rzecz diagnostyki i funkcji zabiegowych. Oddziały łóżkowe stają się działami krótkotrwałego pobytu pacjentów, podstawowe funkcje medyczne przejmują zespoły diagnostyczne i zabiegowe. Postępujący rozwój techniki i technologii medycznej bezpośrednio wpływa na coraz bardziej rozbudowaną...
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IN VITRO PROPAGATION OF RHODODENDRON TOMENTOSUM - AN ENDANGERED ESSENTIAL OIL BEARING PLANT FROM PEATLAND
PublikacjaRhododendron tomentosum Harmaja (formerly Ledum palustre L.) is a medicinal peat bog plant native to northern Europe, Asia and North America. This plant has a distinctive aroma thanks to the presence of essential oil, to which it also owes its anti-inflammatory, analgesic, antimicrobial and insecticidal properties. However, in Europe R. tomentosum is classified as an endangered species, mainly due to degradation of peatlands. In...
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NADZOROWANIE WYPOSAŻENIA DO MONITOROWANIA I POMIARÓW WEDŁUG WYMAGAŃ WYBRANYCH NORM ORAZ PRZEPISÓW PRAWNYCH
Publikacja: Przyrządy pomiarowe stanowią zasadniczy element złożonego systemu oceny jakości wyrobów na wszystkich etapach produkcji. Odpowiednio zaprojektowane procedury opisujące procesy kontrolne i pomiarowe, sprawnie zorganizowane i przeprowadzane operacje monitorowania i pomiarów parametrów procesów i produktów oraz skutecznie funkcjonujący nadzór nad wyposażeniem do monitorowania i pomiarów w organizacji są podstawą do wykazania, że...
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Cadmium and lead content in gluten and gluten-free bread available on the Polish market – potential health risk to consumers
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Zastosowanie techniki ekstrakcji na fazie stałej (SPE) do zagęszczania wielopierścieniowych węglowodorów aromatycznych z płynów stosowanych w infuzji przy oznaczaniu tych związków techniką HPLC z detektorem fluorescencyjnym i diodowym
PublikacjaPraca zawiera metodykę przygotowania próbki oraz procedurę analityczną oznaczania obecności wielopierścieniowych węglowodorów aromatycznych (WWA) w płynach infuzyjnych stosowanych do wlewów dożylnych dla ludzi oraz wyniki badań stężeń tych węglowodorów w płynach stosowanych do infuzji oraz w stosowanych do produkcji płynów infuzyjnych - substancjach farmaceutycznych. W płynach do infuzji stwierdzono 0,2-7,6 ng/l Benzo(a)pirenu,...
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Pomiary impedancji szkliwa zębów w zakresie niskiej częstotliwości.
PublikacjaCelem pracy była ocena in vitro wartości impedancji szkliwa zębów w zakresie niskiej częstotliwości oraz zmian impedancji pod wpływem wilgotności. Pomiarami objęto szkliwo bez zmian, szkliwo z pęknięciami oraz obszary zmienione w wyniku demineralizacji i próchnicy. Wyznaczono zakres zmian impedancji w wymienionych przypadkach.
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Determining ATP concentration in Candida albicans in process of forming germ tube forms
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Ocena stanu antyoksydacyjnego w wybranych chorobach układowych tkanki łącznej
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Księgozbiór profesora Michała Reichera: struktura zasobu
PublikacjaCel pracy Celem niniejszej pracy jest przeprowadzenie analizy zachowanej części księgozbioru prof. M. Reichera zgodne z funkcjonalną koncepcją książki, wedle której daną kolekcję interpretować należy jako wyraz nie tylko zainteresowań i praktyk czytelniczych, ale jako część procesu społecznego komunikowania, rozumianego tutaj jako możność stworzenia kolekcji (kwestie rynku książki) i nadania jej wartości w obiegu informacji naukowej. Materiał...
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Aktywność współczesnych fasad w kontekście rozwoju innowacyjnych technologii
PublikacjaTematem pracy są fasady aktywne. Dążenie do ich tworzenia jest efektem przemian, jakim podlega sama architektura. Wynika także z rozwoju innowacyjnych technologii. W konsekwencji wobec zewnętrznej powłoki budynku stawiane są coraz to nowe wymagania estetyczne i funkcjonalne. Jako odpowiedź na nie, architekci projektują powłoki zewnętrzne reagujące na wpływy środowiska czy ruch użytkownika. Emitują one w przestrzeń miasta fakturalne...
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NEEDS AND CHALLENGES IN DISPATCHING EMERGENCY MEDICAL SERVICES IN SITUATIONS OF POTENTIAL MILITARY DANGER
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Cytochromes P450 and Skin Cancer: Role of Local Endocrine Pathways
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Flavonoids as inhibitors of human neutrophil elastase
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Flavonoids as tyrosinase inhibitors in in silico and in vitro models: basic framework of SAR using a statistical modelling approach
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Synthesis of the inosine 5′-monophosphate dehydrogenase (IMPDH) inhibitors
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SUDDEN CARDIAC ARREST IN PATIENTS OVER 60 YEARS OF AGE IN THE OPERATION AREA OF EMERGENCY MEDICAL SERVICE IN SIEDLCE IN 2013-2017
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LIFE-SAVING PROCEDURES AND CARDIOPULMONARY RESUSCITATION FROM THE ANCIENT HISTORY TO THE PRESENT DAY
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Antiglycoxidative properties of amantadine – a systematic review and comprehensive in vitro study
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Novel synthesis scheme and in vitro antimicrobial evaluation of a panel of (E)-2-aryl-1-cyano-1-nitroethenes
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DIAGNOSES MADE BY LEADERS OF EMERGENCY MEDICA L SERVICES TEAMS WITHIN THE OPERAT ION AREA OF THE EMERGENCY MEDICA L SERVICES STAT ION IN MINSK MAZOWIECKI IN 2013-2017
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Synthesis and biological activity of ester derivatives of mycophenolic acid and acridines/acridones as potential immunosuppressive agents
PublikacjaImproved derivatives of mycophenolic acid (MPA) are necessary to reduce the frequency of adverse effects, this drug exerts in treated patients. In this study, MPA was coupled with N-(x-hydroxyalkyl)-9-acridone-4-carboxamides or N-(x-hydroxyalkyl)acridine-4-carboxamides to give respective ester conjugates upon Yamaguchi protocol. This esterification required protection of phenol group in MPA. Designed conjugates revealed higher...
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9,10-Dioxoanthracenyldithiocarbamates effectively inhibit the proliferation of non-small cell lung cancer by targeting multiple protein tyrosine kinases
PublikacjaAnthraquinones have attracted considerable interest in the realm of cancer treatment owing to their potent anticancer properties. This study evaluates the potential of a series of new anthraquinone derivatives as anticancer agents for non-small-cell lung cancer (NSCLC). The compounds were subjected to a range of tests to assess their cytotoxic and apoptotic properties, ability to inhibit colony formation, pro-DNA damage functions,...
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Development of potent and effective SARS-CoV-2 main protease inhibitors based on maleimide analogs for the potential treatment of COVID-19
PublikacjaIn 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 SARS-CoV-2). Within the set of new Mpro inhibitors, 6e demonstrated the highest activity in the enzymatic assay with an IC50 value of 8.52 ± 0.44 mM. The IC50 value for Nirmatrelvir (PF-07321332,...
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Palindromic carbazole derivatives: unveiling their antiproliferative effect via topoisomerase II catalytic inhibition and apoptosis induction
PublikacjaHuman DNA topoisomerases are essential for crucial cellular processes, including DNA replication, transcription, chromatin condensation, and maintenance of its structure. One of the significant strategies employed in cancer treatment involves the inhibition of a specific type of topoisomerase, known as topoisomerase II (Topo II). Carbazole derivatives, recognised for their varied biological activities, have recently become a significant...
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Recent progress in the development of steroid sulfatase inhibitors – examples of the novel and most promising compounds from the last decade
PublikacjaThe purpose of this review article is to provide an overview of recent achievements in the synthesis of novel steroid sulfatase (STS) inhibitors. STS is a crucial enzyme in the biosynthesis of active hormones (including estrogens and androgens) and, therefore, represents an extremely attractive molecular target for the development of hormone-dependent cancer therapies. The inhibition of STS may effectively reduce the availability...
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New potent steroid sulphatase inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives
PublikacjaIn 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-triazol-4-yl)naphthalen-2-yl sulphamate 3L demonstrated the highest activity in the enzymatic assay inhibiting the STS activity to 7.98% at 0.5 µM concentration. Furthermore, to verify...
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Anticancer Properties of Amino Acid and Peptide Derivatives of Mycophenolic Acid
PublikacjaBackground: Although Mycophenolic Acid (MPA) is applied as prodrugs in clinic as an immunosuppressant, it also possesses anticancer activity. MPA acts as Inosine-5’-Monophosphate Dehydrogenase (IMPDH) inhibitor, where the carboxylic group at the end of the side chain interacts with Ser 276 of the enzyme via hydrogen bonds. Therefore, MPA derivatives with other polar groups indicated high inhibition too. On the other hand, potent...
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Novel amides of mycophenolic acid and some heterocyclic derivatives as immunosuppressive agents
PublikacjaThe group of new amide derivatives of mycophenolic acid (MPA) and selected heterocyclic amines was synthesised as potential immunosuppressive agents functioning as inosine-5'-monophosphate dehydrogenase (IMPDH) uncompetitive inhibitors. The synthesis employed uronium-type activating system (TBTU/HOBt/DIPEA) while or phosphonic acid anhydride method (T3P/Py) facilitating amides to be obtained in moderate to excellent yields without...