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Wyniki wyszukiwania dla: BISACRIDINE DERIVATIVES
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Chapter 22. Antimicrobial and surface activity of 1-alkyl-3-methyl imidazolium derivatives
PublikacjaCiecze jonowe wykazują aktywność przeciwgrzybową oraz przeciwbakteryjną zależną od struktury badanego związku. Zbadano wpływ długości łańcucha alkilowego w kationie na aktywność przeciwmikrobiologiczną oraz przedstawiono zależność pomiędzy tą aktywnością a krytycznym stężeniem micelizacji imidazolowych cieczy jonowych.
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Influence of a lipid bilayer on the conformational behavior of amphotericin B derivatives - A molecular dynamics study.
PublikacjaAmphotericin B (AmB) is an effective but very toxic antifungal antibiotic. In our laboratory a series of AmB derivatives of improved selectivity of action was synthesized and tested. To understand molecular basis of this improvement, comparative conformational studies of amphotericin B and its two more selectivederivatives were carried out in an aqueous solution and in a lipid membrane. These molecular simulation studies revealed...
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Synthesis of conjugates of muramyl dipeptide and nor-muramyl dipeptide derivatives with adenosine as potential immunosuppressant
PublikacjaZaprezentowano syntezę koniugatów adenozyny z pochodnymi muramylo- i nor-muramylodipeptydów zawierających w części peptydowej D-aminokwasy (D-Ala, D-Val, D-Ser, D-Pro, D-2-ABA). Jako substrat zastosowano rybozyd 6-chloropuryny, który łączono poprzez 1,2-diaminoetan z odpowiednimi pochodnymi MDP lub nor-MDP w obecności EDCI i HOBt. Struktury otrzymanych związków zostały potwierdzone widmami 1H i 13C NMR (500 MHz), widmami MS oraz...
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Synthesis of conjugates of muramyl dipeptide and nor-muramyl dipeptide derivatives with adenosine as potential immunosuppressants
PublikacjaPrzedstawiono syntezę koniugatów pochodnych muramylodipeptydu (MDP) i nor-MDP z adenozyną jako potencjalnych związków o działaniu immunosupresyjnym. Jako substrat zastosowano rybozyd 6-chloropuryny, który łączonp poprzez 1,2-diaminoetan z pochodną MDP lub nor-MDP. Do syntezy wykorzystano pochodne MDP zawierające w części peptydowej D-aminokwasy (D-Ala, D-Val, D-Ser, D-Pro, D-2-ABA). Jako odczynniki sprzęgające zastosowano EDCI...
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Synthesis of phosphono and phosphate derivatives of hydroxyimino-D-alditols as new potential antifungal agents
PublikacjaIn search for new effective we antyfungals we focus on two enzymes involved in biosynthesis of the fungal cell wall. The first enzyme is glucosamine-6-phosphate (GlmS), which catalyzes transformation of D-fructose-6-phosphate (Fru-6P) to D-glucosamine-6-phodphate (GlcN-6P) in the chitin biosynthesis pathway. The second enzyme is phosphomannose isomerase (PMI) repored to play a crucial role in biosynthesis of many mannosylated structures,...
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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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Synthesis and antimicrobial activity of 6-sulfo-6-deoxy-D-glucosamine and its derivatives
Publikacja6-Sulfo-6-deoxy-D-glucosamine (GlcN6S), 6-sulfo-6-deoxy-D-glucosaminitol (ADGS) and their N-acetyl and methyl ester derivatives have been synthesized and tested as inhibitors of enzymes catalyzing reactions of the UDP-GlcNAc pathway in bacteria and yeasts. GlcN6S and ADGS at micromolar concentrations inhibited glucosamine-6-phosphate (GlcN6P) synthase of microbial origin. The former was also inhibitory towards fungal GlcN6P N-acetyl...
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Monosubstituted hydrazone β-cyclodextrin derivatives for pH-sensitive complex formation with aromatic drugs
PublikacjaA new and convenient synthetic pathway was developed to produce monosubstituted cyclodextrins with high yields. Each of the β-cyclodextrin derivatives described in this work has an aromatic substituent connected with cyclodextrin core by a pH-sensitive hydrazone linker and a carbon chain. Carbon chains differ in lengths having one or three carbon atoms. The correlation between water solubility and linker length was determined using...
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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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Thermal Decomposition of Carbamoyl Meldrum’s Acids: A Starting Point for the Preparation of 1,3-Oxazine Derivatives
PublikacjaThe ability to undergo [4 + 2] versus [2 + 2] cycloaddition was under investigation for ketenes thermally generated from carbamoyl Meldrum’s acid. Usually, 1,3-oxazino-5-carbamoylo-4,6-diones are formed when carbamoyl Meldrum’s acid reacts with imine. However, in some cases, a reaction takes an unexpected course, leading to the formation of tetraponerines alkaloids derivatives or cyclic iminoethers.
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Effect of thienyl units in cyanoacrylic acid derivatives toward dye-sensitized solar cells
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Preliminary antifungal activity assay of selected chlorine-containing derivatives of xanthone and phenoxyethyl amines
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Conformational Preferences of Proline Derivatives Incorporated into Vasopressin Analogues: NMR and Molecular Modelling Studies
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Structure–bioavailability relationship study of genistein derivatives with antiproliferative activity on human cancer cell
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Synthesis of New Hydrazone Derivatives and Evaluation of their Efficacy as Proliferation Inhibitors in Human Cancer Cells
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Anticancer properties of ester derivatives of betulin in human metastatic melanoma cells (Me-45)
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Chromane helicity rule – scope and challenges based on an ECD study of various trolox derivatives
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Two novel nucleoside ester derivatives of chlorambucil as potential antileukemic prodrugs: a preliminary study
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Synthesis and photo-conversion of androsta- and pregna-5,7-dienes to vitamin D3-like derivatives
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Solvent effects on fluorescence properties of protochlorophyll and its derivatives with various porphyrin side chains
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Chemometric analysis of UV-Vis spektra of associated forms of Amphotericin B and its derivatives
PublikacjaPrzedmiotem badań był proces agregacji nowych pochodnych antybiotyku polienowego Amfoterycyny B. Do śledzenia procesu agregacji wykorzystano spektroskopię absorpcyjną w zakresie widzialnym i bliskiego nadfioletu. Zastosowanie zaawansowanych technik chemometrycznych pozwoliło na dogłębną analizę agregacji tych pochodnych, co pozwoliło na wyciągniecie następujacych wniosków: i) w przypadku wszystkich pochodnych przy stężeniach poniżej...
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Skin cancer, including related pathways and therapy and the role of luteolin derivatives as potential therapeutics
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Pharmacological Profile and Molecular Modeling of Cyclic Opioid Analogues Incorporating Various Phenylalanine Derivatives
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Synthesis of functionalized new conjugates of batracylin with tuftsin/ retro-tuftsin derivatives and their biological evaluation
PublikacjaNew batracylin conjugates with tuftsin/retro-tuftsin derivatives were designed and synthesized using T3P as a coupling agent. The conjugates possess an amide bond formed between the carboxyl group of heterocyclic molecule and the N-termini of the tuftsin/retro-tuftsin chain. The in vitro cytotoxic activity of the new analogues and their precursors was evaluated using a series of human and murine tumor cells. BAT conjugates containing...
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Effect of chemical structure on complexation efficiency of aromatic drugs with cyclodextrins: The example of dibenzazepine derivatives
PublikacjaIt is widely believed that the hydrophobic effect governs the binding of guest molecules to cyclodextrins (CDs). However, it is also known that high hydrophobicity of guest molecules does not always translate to the formation of stable inclusion complexes with CDs. Indeed, a plethora of other factors can play a role in the efficiency of guest–CD interactions, rendering structure-based prediction of the complexation efficiency with...
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Novel N-(aryl/heteroaryl)-2-chlorobenzenesulfonamide derivatives: synthesis and anticancer activity evaluation
PublikacjaA new series of N-(aryl/heteroaryl)-2-chlorobenzenesulfonamide derivatives 4-21 have been synthesized, and evaluated at the National Cancer Institute (USA) for their in vitro activities against a panel of 60 different human cancer cell lines. Among them, compounds 16, 20 and 21 exhibited remarkable cytotoxic activity against numerous human cancer cell lines. We found that sulfonamide derivative 21 appeared to be more selective...
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Tetrahydroquinolinone derivatives exert antiproliferative effect on lung cancer cells through apoptosis induction
PublikacjaThe anticancer properties of quinolones is a topic of interest among researchers in the scientific world. Because these compounds do not cause side effects, unlike the commonly used cytostatics, they are considered a promising source of new anticancer drugs. In this work, we designed a brief synthetic pathway and obtained a series of novel 8-phenyltetrahydroquinolinone derivatives functionalized with benzyl-type moieties at position...
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Improving the regulation of the derivatives market as an objective prerequisite for sustainable development of the global financial system
PublikacjaThe development of financial markets is characterized by the emergence of new financial instruments, in particular derivatives, the risk level analysis of which is complicated. Counterparties are not always fully aware of and do not adequately assess the potential risks of derivatives, which may lead to large financial losses and sometimes bankruptcies. The purpose of the study is to generalize approaches to regulating derivative...
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Photoresponsive Amide-Based Derivatives of Azobenzene-4,4′-Dicarboxylic Acid—Experimental and Theoretical Studies
PublikacjaAzobenzene derivatives are one of the most important molecular switches for biological and material science applications. Although these systems represent a well-known group of compounds, there remains a need to identify the factors influencing their photochemical properties in order to design azobenzene-based technologies in a rational way. In this contribution, we describe the synthesis and characterization of two novel amides...
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The products of electro- and photochemical oxidation of 2-hydroxyacridinone, the reference compound of antitumor imidazoacridinone derivatives
PublikacjaBadano reakcje elektrochemicznego utleniania 2-hydroksyakrydonu, związku modelowego aktywnych przeciwnowotworowo pochodnych imidazoakrydonu. Do badań zastosowano metody woltamperometrii cyklicznej, metodę spektroelektrochemiczną oraz elektrolizę przy kontrolowanym potencjale. Badano też reakcje fotochemicznego utleniania. Badania prowadzono w ramach szerszego problemu poznania przemian aktywacji metabolicznej pochodnych hydroksyakrydonu...
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Indole-Acrylonitrile Derivatives as Potential Antitumor and Antimicrobial Agents—Synthesis, In Vitro and In Silico Studies
PublikacjaA series of 2-(1H-indol-2-yl)-3-acrylonitrile derivatives, 2a–x, 3, 4a–b, 5a–d, 6a–b, and 7, were synthesized as potential antitumor and antimicrobial agents. The structures of the prepared compounds were evaluated based on elemental analysis, IR, 1H- and 13NMR, as well as MS spectra. X-ray crystal analysis of the representative 2-(1H-indol-2-yl)-3-acrylonitrile 2l showed that the acrylonitrile double bond was Z-configured. All...
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Xanthone synthetic derivatives with high anticandidal activity and positive mycostatic selectivity index values
PublikacjaWith the current massive increases in drug-resistant microbial infection as well as the significant role of fungal infections in the death toll of COVID-19, discovering new antifungals is extremely important. Natural and synthetic xanthones are promising derivatives, although only few reports have demonstrated their antifungal mechanism of action in detail. Newly synthetized by us xanthone derivative 44 exhibited strong antifungal...
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In vitro enzyme kinetics and NMR-based product elucidation for glutathione S-conjugation of the anticancer unsymmetrical bisacridine C-2028 in liver microsomes and cytosol: major role of glutathione S-transferase M1-1 isoenzyme
PublikacjaThis work is the next step in studying the interplay between C-2028 (anticancer-active unsymmetrical bisacridine developed in our group) and the glutathione S-transferase/glutathione (GST/GSH) system. Here, we analyzed the concentration- and pH-dependent GSH conjugation of C-2028 in rat liver microsomes and cytosol. We also applied three recombinant human GST isoenzymes, which altered expression was found in various tumors. The...
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Non-enzymatic glutathione-mediated conjugation of unsymmetrical bisacridine C-2028 with anticancer activity
Dane BadawczeThe presented data complement the studies on the interplay between C-2028 (anticancer-active unsymmetrical bisacridine) and the glutathione S-transferase/glutathione (GST/GSH) system.
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Addendum to ''On the derivative of the Legendre function of the first kind with respect to its degree''
PublikacjaPraca stanowi uzupełnienie wcześniejszej publikacji autora [J. Phys. A: Math. Gen. 39(2006) 15147-15172]. Przedstawiono w niej nowe wyrażenia dla pochodnej funkcji Legendre'a względem jej indeksu i zastosowano je do konstrukcji dwóch nowych reprezentacji funkcji Legendre'a drugiego rodzaju z całkowitym indeksem.
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Existence and uniqueness for neutral equations with delay dependant on a solution and its derivative
PublikacjaDla wykazania istnienia i jednoznaczności w pracy została zaprezentowana metoda porównawcza.
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Proportional-derivative and Model-based Controllers for Control of a Variable Mass Manipulator
PublikacjaW artykule prezentowano wyniki analiza numeryczna dynamiki manipulatora o zmiennej masie. W skład manipulatora wchodzą jedynie członu i przeguby obrotowe. Ładowność chwytaka jest traktowana jako jedyny element o zmiennej masie. Podobnie jak w przypadku innych manipulatorów wyposażonych w przeguby obrotowe, parametry jego dynamika zależą od aktualnego ustawienia. Gdy przemieszczenia obejmują większy zakres roboczy, w równaniach...
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Proportional-Derivative and Model-Based Controllers for Control of a Variable Mass Manipulator
PublikacjaIn the paper, numerical analysis of dynamics of a variable mass manipulator is presented. A revolute joints composed manipulator is considered. Payload of the gripper is considered as the only element characterized by unknown value of its mass (variable between subsequent operations). As in other cases of the revolute joints composed manipulators, its behaviour dependents significantly on the pose of the manipulator. When the manipulator...
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A NUMERICAL STUDY ON THE DYNAMICS OF DENGUE DISEASE MODEL WITH FRACTIONAL PIECEWISE DERIVATIVE
PublikacjaThe aim of this paper is to study the dynamics of Dengue disease model using a novel piecewise derivative approach in the sense of singular and non-singular kernels. The singular kernel operator is in the sense of Caputo, whereas the non-singular kernel operator is the Atangana–Baleanu Caputo operator. The existence and uniqueness of a solution with piecewise derivative are examined for the aforementioned problem. The suggested...
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Signal Propagation in Electromagnetic Media Modelled by the Two-Sided Fractional Derivative
PublikacjaIn this paper, wave propagation is considered in a medium described by a fractional-order model, which is formulated with the use of the two-sided fractional derivative of Ortigueira and Machado. Although the relation of the derivative to causality is clearly specified in its definition, there is no obvious relation between causality of the derivative and causality of the transfer function induced by this derivative. Hence, causality...
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Pochodne kwasu neopentylidenofosforoditiowego jako substraty do syntezy ugrupowania trisulfidowego
PublikacjaBadania przeprowadzone w Katedrze Chemii Organicznej Wydziału Chemicznego Politechniki Gdańskiej na przestrzeni ostatnich kilku lat, pokazały wszechstronność pochodnych kwasu neopentylidenofosforoditiowego [32] w syntezie symetrycznie i niesymetrycznie podstawionego ugrupowania disulfidowego. Wyniki powyższych badań doprowadziły do opracowania nowej strategii syntetycznej, umożliwiającej otrzymywanie...
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Chromogenic complexes and selective preconcentration of Fe(III) and Cu(II) by hydroxynaphthoyl-1,4,7,10-tetraazacyclododecane derivatives
PublikacjaSpektroskopowe oznaczanie zawartości jonów żelaza w różnych próbkach środowiskowych jest przedmiotem wieloletnich badań. Pomimo tego ciągle poszukuje się selektywnych odczynników zdolnych do tworzenia kompleksów z jonami żelaza(II) lub żelaza(III). 1,4,7,10-tetraazacyklododekan nie tworzy kompleksów z jonami żelaza, ale wprowadzając stosowne podstawniki można uzyskać właściwe ligandy. W reakcji acylowania otrzymano 1-(1-hydroksy-2-naftoilo)-1,4,7,10-tetraazacyklododekan...
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Estimation of interior-permanent-magnet-synchronous-motor rotor position by analysis of phase-current derivatives
PublikacjaThis paper describes an algorithm for estimation of IPMSM rotor angular position. The algorithm uses derivatives of motor phase currents resulting from PWM modulation to obtain the rotor position. The presented method is designed for medium- and high-speed range, since it is based on determination of the EMF vector. Calculation of the motor position is performed in every PWM cycle. The standard SV-PWM method is used to determine...
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Carboxymethylated starch and cellulose derivatives-based film as human skin equivalent for adhesive properties testing
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The organophosphorus sulfenyl bromides as versatile reagents for cysteine derivatives functionalization by unsymmetrical disulfide bond formation
PublikacjaWe have developed a convenient method for the synthesis of L-cysteine unsymmetrical disulfides under mild conditions with good to excellent yields. Described method is based on the straightforward preparation of the organophosphorus sulfenyl bromide readily available from bis-(5,5-dimethyl-2-thiono-1,3,2-dioxaphosphorinanyl) disulfide. The unsymmetrical disulfides can be obtained for L-cysteine derivatives and thiols bearing neutral...
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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 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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Molecular modeling and evaluation of novel dibenzopyrrole derivatives as telomerase inhibitors and potential drug for cancer therapy
PublikacjaDuring previous years, many studies on synthesis, as well as on anti-tumor, anti-inflammatory and anti-bacterial activities of the pyrazole derivatives have been described. Certain pyrazole derivatives exhibit important pharmacological activities and have proved to be useful template in drug research. Considering importance of pyrazole template, in current work the series of novel inhibitors were designed by replacing central...
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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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Inactivation of glucosamine-6-phosphate synthase by N3-oxoacyl derivatives of L-2,3-diaminopropanoic acid
PublikacjaN3-oksoacylowe pochodne kwasu l-2,3-diaminopropanowego zawierające ugrupowanie epoksydowe lub układ sprzężonych wiązań podwójnych inaktywują syntaze glukozamino-6-fosforanu (GlcN-6-P) z S. cerevisiae. Wyniki badań kinetycznych inaktywacji enzymu wskazują na dwuetapowy przebieg tej reakcji, przy czym tworzenie kompleksu enzym:ligand poprzedza nieodwracalną modyfikację enzymu. Badane związki różniły się powinowactwem do centrum aktywnego...