Wyniki wyszukiwania dla: bis-phosphonic acid derivatives, one-pot synthesis
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Opracowanie dogodnej metody tworzenia wiązań S-C o hybrydyzacji atomu węgla sp oraz sp2
PublikacjaBadania przeprowadzone w Katedrze Chemii Organicznej Wydziału Chemicznego Politechniki Gdańskiej na przestrzeni ostatnich kilku lat, pokazały wszechstronność pochodnych kwasu neopentylidenofosforoditiowego. Dotychczasowe wyniki badań doprowadziły mnie do opracowania nowych strategii syntetycznych, umożliwiających otrzymywanie związków zawierających wiązanie C-S o hybrydyzacji atomu węgla sp oraz sp2. Analizując wyniki badań opracowałam...
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Fully scalable one-pot method for the production of phosphonic graphene derivatives
PublikacjaGraphene oxide was functionalized with simultaneous reduction to produce phosphonated reduced graphene oxide in a novel, fully scalable, one-pot method. The phosphonic derivative of graphene was obtained through the reaction of graphene oxide with phosphorus trichloride in water. The newly synthesized reduced graphene oxide derivative was fully characterized by using spectroscopic methods along with thermal analysis. The morphology...
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Bis-phosphonated carbon nanotubes: one pot synthesis and their application as efficient adsorbent of mercury
PublikacjaEffective, one-pot method of CNTs phosphonylation is presented. Cheap and readily available reagents are used, so the process can be easily transferred to large-scale production. The product was analyzed using spectroscopic methods (FTIR, UV-vis, XPS). Thermal properties of the bis-phosphonated nanotubes are reported for the first time. Newly obtained material was tested as an adsorbent for mercury removal from water. The sorption...
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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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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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Acyl Meldrum's acid derivatives: application in organic synthesis
PublikacjaThis review is focused on one of the most important classes of Meldrum's acid derivatives commonly known as acyl Meldrum's acids. The preparation methods of these compounds are considered including the recently proposed and rather rarely used ones. The chemical properties of acyl Meldrum's acids are described in detail, including thermal stability and reactions with various nucleiophiles. The possible mechanisms of these transformations...
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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...
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Chromogenic derivatives of new bis(phenylhydrazono-1H-tetrazol-5-yl-acetonitriles) - synthesis and properties
PublikacjaDerivatives of bis(phenylhydrazono-1H-tetrazol-5-yl-acetonitriles) with oxygen and sulphur atoms in the structure of aliphatic chains were successfully synthesised. The correlation between the ligand structure and its complexation properties was investigated by absorption spectroscopy. The formation of complexes of presented compounds with metal cations (Cu2+, Ni2+, Zn2+, Co2+, Fe2+ and Pb2+) was studied. Ligands 5-8 were additionally...
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Synthesis and antiproliferative activity of new mycophenolic acid conjugates with adenosine derivatives
PublikacjaNew conjugates of mycophenolic acid (MPA) and adenosine derivatives were synthesized and assessed as potential immunosuppressants on Jurkat cell line and peripheral blood mononuclear cells (PBMC) from healthy donors. As compared to MPA, all compounds were found to be more active against Jurkat cell line. The antiproliferative activities were compared with MPA and adenosine, in both 2′,3′-O-isopropylidene protected and free hydroxyl...
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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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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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Synthesis and biological activity of mycophenolic acid-amino acid derivatives
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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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Catalytic Asymmetric Synthesis of Isochroman Derivatives
PublikacjaThe isochroman scaffold constitutes an important structural unit, which is present in various bioactive natural products and synthetic pharmaceutical compounds exhibiting wide arrays of biological properties. Hence the synthesis of this class of heterocyclic compounds in a stereoselective fashion is highly significant and desirable. In the last decade, a substantial advancement has been witnessed ln the catalytic asymmetric...
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Modifications of total synthesis of mycophenolic acid
PublikacjaThe total synthesis of mycophenolic acid (MPA), a potent immunosuppressant, was modified. The obtained mycophenolic acid was suitable for further preparation of new prospective immunosuppressants with improved therapeutic properties.
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Synthesis of thiol derivatives of azobenzocrown ethers. The preliminary studies on recognition of alkali metal ions by gold nanoparticles functionalized with azobenzocrown and lipoic acid
PublikacjaThe article presents the synthesis of novel 13- and 16-membered azobenzocrown derivatives with peripheral thiol moieties and preliminary studies assessing their possible application in plasmonic sensors based on gold nanoparticles. The effect of the length of the chain connecting the macrocycle with the thiol group and the effect of the presence of the additional functional compound,...
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NADES propolis extracts - update 2023 and synthesis of derivatives of propolis ingredients
Dane BadawczeThis dataset contains results of our investigation aiming in determination of antimicrobial potential of the propolis extracts produced with deep eutectic solvents
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Synthesis of disubstituted 1,3,4,9-tetrahydropyrano-[3,4-b]indole-1-acetic acids derivatives
Publikacja1,3,4,9-tetrahydropyrano[3,4-b ]indole-1-acetic acid derivatives are of interest for pharmaceutical research as a core structure for synthesis of biological active substance - Etodolac (selective Cyclooxygenase-2 inhibitor, which belongs to the Non-steroidal Anti-inflammatory Drug, NSAID, that shows a clin-ically effective analgesic and anti-inflammatory activity). Here the way of synthesis of two 1,3,4,9-tetrahydropyrano[3,4-b...
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Amino Acid Based Antimicrobial Agents – Synthesis and Properties
PublikacjaStructures of several dozen of known antibacterial, antifungal or antiprotozoal agents are based on the amino acid scaffold. In most of them, the amino acid skeleton is of a crucial importance for their antimicrobial activity, since very often they are structural analogs of amino acid intermediates of different microbial biosynthetic pathways. Particularly, some aminophosphonate or aminoboronate analogs of protein amino acids are...
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Investigations on the immunosuppressive activity of derivatives of mycophenolic acid in immature dendritic cell
PublikacjaThe main activity of mycophenolic acid (MPA) and its analogs is the inhibition of proliferation of T cells. Here, we hypothesized that MPA and its conjugates inhibits also the activity of antigen-presenting cells (APC) including dendritic cells (DCs). We tested the effect of novel amino acid derivatives of MPA and conjugates of MPA with acridines/acridones on DCs by flow cytometry, ELISA and MLR assay. Both acridines/acridone derivatives...