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Search results for: b-lactams
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One-Step Synthesis of b-Lactams with Retro-Amide Side Chain
PublicationAbstract: A one pot synthesis for preparation of 1,4-disubstituted-2-oxo-azetidine-3-carboxylic acid amides was developed. 5-(α-N-substituted-amino-α'-hydroxy)methylene Meldrum's acids act as a source of ketenes that react with aldimines in boiling toluene to give b-lactams with retro-amid side chain.
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Synthesis of 3-Carbamoyl b-Lactams via Manganese(III)-Promoted Cyclization of N-Alkenylmalonamides
PublicationManganese(III)-promoted cyclization of N-alkenylmalonamides (¼N-alkenylpropanediamides) gave 3-(aryl/(alkylamino)carbonyl) b-lactams as well as 3-(aryl/(alkylamino)thiocarbonyl) b-lactams. The relative configuration of the obtained products was unambiguously determined by X-ray crystallography. The proposed method is very useful for the one-pot synthesis of a number of 3-(aryl/ (alkylamino)carbonyl) b-lactams, especially those...
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A new approach to the stereoselective synthesis of trans-3-carbamoyl-b-lactam moieties†
PublicationOne-pot synthesis of optically active 1,4-disubstituted-3-carbamoyl-azetidinones from 5-[(N-arylamino)- (hydroxyl)methylene]-2,2-dimethyl-1,3-dioxa-4,6-diones and chiral aldimines is achieved via thermal generation of carbamoyl ketenes and subsequent [2+2] cycloaddition. Three possible chiral induction approaches were tested and (R)-(+)-1-phenylethylamine was confirmed as the best chiral auxiliary. Among the four possible diastereoisomers,...
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Studies on the complex formation between lactams and thiolactams of sparteine with copper(II) cation
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Simple and novel synthesis of 3-(thio)phosphoryl-β-lactams by radical cyclization
PublicationRadical cyclization of phosphono-acetenamides promoted by manganese(III) acetate leads exclusively to the formation of 3-phosphoryl-β-lactams. The thiophosphoryl analogues were also prepared using this method. In particular, the presented protocol does not require the use of noble metals, while comparable methods do.
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<b><i>CTLA4</i></b> and <b><i>CD28</i></b> Gene Polymorphisms with Respect to Affective Symptom Domain in Schizophrenia
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Convenient synthesis of 3-phosphono-β-lactams through the cyclization ofN-alkenyl-phosphonoacetamides
PublicationOxidative cyclization through the treatment by the transition metals is convenientsynthetic tool with a great number of applications. In the most cases the result is the formationof C-C bond between generated radical and unsaturated part of the same or another molecule.As it was presented by Trogolo it is also suitable way to obtain 4-membered heterocyclicβ-lactamic ring[1]. In this communicate we want to present new application...
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Synthesis of Polycyclic δ-Lactams with Bridged Benzomorphan Skeleton: Selectivity and Diversity Driven by Substituents
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Węzły grupy B
PublicationWęzły grupy B są budowane na przecięciach dróg, z których jedna - z definicji - nie może mieć punktów kolizji, na drugiej natomiast są one dopuszczalne. Węzeł taki oznacza zazwyczaj połączenie drogi ruchu szybkiego z drogami podrzędnymi. Oczywiście, nawet na przecięciu dróg ogólnodostępnych może być zastosowany węzeł grupy A - czyli węzeł całkowicie bezkolizyjny, o ile natężenia i ranga krzyżujących się dróg uzasadniają przyjecie...
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A Holistic Approach to Determining Stereochemistry of Potential Pharmaceuticals by Circular Dichroism with β-Lactams as Test Cases
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The stereoselective formation of β-lactams with acyl ketenes generated from 5-acyl-Meldrum's acids
PublicationAcyl ketenes formed during thermal decompositions of 5-acyl-2,2-dimethyl-1,3-dioxa-4,6-diones undergo stereoselective [2+2] cycloaddition to chiral aldimines. We report the first example of optically active 3-acyl-β-lactams formation from Meldrum’s acid derivatives.
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Manganese(III) Promoted Cyclization of N-alkenyl-N-(2-hydroxyethyl) amides to Iso-Oxacepham Potent β-Lactamase Inhibitors
PublicationBackground: β-Lactams are still a subject of interest of organic chemists. The main reason for this interest is due to their application as a chemotherapeutic. β-Lactam antibiotics are still the most commonly used drugs in bacterial infections. Method: Methods using 4-exo-trig radical cyclization leading to β-lactams are an alternative to classical Staudinger`s β-Lactams formation. We prepared N-alkenyl-N-(2-hydroxyethyl)amides...
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Structure elucidation of carbamoylo-β-lactam diastereoisomers by ROESY and NOESY experiments
PublicationRecently we have focused in the problem of preparation of carbamoylo-β-lactams as a result of oxidative cyclization of malonyl enamides. In our experiments we obtain mixture of two main β-lactam products: as a result of subsequent elimination and a second as a product of substitution. All of the produced β-lactams have trans configuration what was confirmed by 1H coupling constants. However id should be stressed that in the case...
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Thermal properties of terpoly(ester-b-ether-b-amide)s with aliphatic ester blocks
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Single-Step Symmetrical Double Alkylation of β,γ-Unsaturated δ-Lactams via Magnesium ‘Ate’ Complexes
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Regulation of carbon catabolism in Lactococcus lactis
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TaRh 2 B 2 and NbRh 2 B 2 : Superconductors with a chiral noncentrosymmetric crystal structure
PublicationIt is a fundamental truth in solid compounds that the physical properties follow the symmetry of the crystal structure. Nowhere is the effect of symmetry more pronounced than in the electronic and magnetic properties of materials—even the projection of the bulk crystal symmetry onto different crystal faces is known to have a substantial impact on the surface electronic states. The effect of bulk crystal symmetry on the properties...
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Stereochemical Assingment of β -lactam Antibiotics and their Analogues by Electronic Circular Dichroism Spectroscopy
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Characterization and Wear Response of Magnetron Sputtered W–B and W–Ti–B Coatings on WC–Co Tools
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Application of gas chromatography to the study of the kinetics of reactionsin solution. Ring opening reactions for á-lactams studied using internal standard
PublicationW pracy przedstawiono metodę badania kinetyki reakcji otwarcia pierścienia á-laktamu, wykorzystującą technikę chromatografii gazowej. Na podstawie badań kinetyki reakcji w różnych temperaturach wyznaczono wartości energii aktywacji dwóch badanych reakcji. Podstawowym celem pracy było pokazanie możliwości wykorzystania GC w badaniach kinetyki reakcji prowadzonych w mikroskali.
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The influence of chemical composition of amide block on the thermal properties and structure of terpoly(ester-b-ether-b-amide) elastomers
PublicationMultiblock terpolymers-(PBT-b-PTMO-b-PA12,10)(n)- constituting the polymer systems, in which one of the three blocks (PBT) does not dissolve in PA12,10 block (hard phase) and, depending on its molecular weight is slightly soluble in PTMO block (soft phase), have been obtained. The DSC method was applied to investigate the thermal properties of these polymers and it was found that PBT block acts as an element that produces stiffness...
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Electron collision with B(CD3)3 molecules
PublicationArtykuł prezentuje całkowite przekroje czynne na rozpraszanie elektronów na drobinach B(CD3)3 zmierzone dla niskich i średnich energii zderzenia. Wyniki porównano z elastycznymi i jonizacyjnymi przekrojami czynnymi obliczonymi dla drobiny B(CD3)3 dla średnich energii zderzenia. Porównano i przedyskutowano przekroje czynne dla drobin zawierających bor.
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Production and characterization of MWBNNT and B-doped SWCNT
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A Zn-Dependent Metallopeptidase Is Responsible for Sensitivity to LsbB, a Class II Leaderless Bacteriocin of Lactococcus lactis subsp. lactis BGMN1-5
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The Lack of Association between <b><i>FCN2</i></b> Gene Promoter Region Polymorphisms and Dental Caries in Polish Children
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Alternative Lactose Catabolic Pathway in Lactococcus lactis IL1403
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Activation of N2O and SO2 by the P–B Bond System. Reversible Binding of SO2 by the P–O–B Geminal Frustrated Lewis Pair
PublicationHerein, we present the first transformation of borylphosphine into borylphosphinite using nitrous oxide. Borylphosphine reacts with N2O via insertion of a single oxygen atom into the P−B bond and formation of a P−O−B bond system. Borylphosphine and borylphosphinite capture SO2 and activate it in an irreversible and reversible manner, respectively.
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NbIr 2 B 2 and TaIr 2 B 2 – New Low Symmetry Noncentrosymmetric Superconductors with Strong Spin–Orbit Coupling
PublicationSuperconductivity was first observed more than a century ago, but the search for new superconducting materials remains a challenge. The Cooper pairs in superconductors are ideal embodiments of quantum entanglement. Thus, novel superconductors can be critical for both learning about electronic systems in condensed matter and for possible application in future quantum technologies. Here two previously unreported materials, NbIr2B2...
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Preparation and photocatalytic activity of B-doped titanium dioxide
PublicationOtrzymano TiO2 domieszkowany borem, aktywny w reakcjach fotodegradacji pod wpływem światła widzialnego (λ>400 nm). Fotokatalizatory otrzymano poprzez hydrolizę tytanianu(IV) izopropylu w obecności związków boru lub poprzez ucieranie ST-01 z prekursorami B i następnie kalcynację w temperaturze 450stC. Jako źródło boru zastosowano kwas borowy (0,5 i 10%wag.) lub trietylo ester kwasu borowego (0,5; 1; 5 i 10%wag.). Najwyższą aktywność...
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Ni2X2 (X=pnictide, chalcogenide, or B) based superconductors
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Genetic Variability of Hepatitis B Virus Isolates in Poland
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Ipertrofan Revisited—The Proposal of the Complete Stereochemistry of Mepartricin A and B
PublicationBeing a methyl ester of partricin, the mepartricin complex is the active substance of a drug called Ipertrofan (Tricandil), which was proven to be useful in treatment of benign prostatic hyperplasia and chronic nonbacterial prostatitis/chronic pelvic pain syndrome. Nevertheless, no direct structural evidence on the stereochemistry of its components has been presented to date. In this contribution, we have conducted detailed, NMR-driven...
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Novel primosomal protein B from Clostridium pastuerianum
PublicationPriB is a primosomal protein that catalyzes DNA replication in Procaryota. The replication pathway starts with PriA protein - the initiator protein that binds to a DNA replication fork, unwinds double-stranded DNA and role of PriB is to stabilize PriA on the DNA. However there are many biochemical differences in replication mechanism in bacteria and only some of them use PriB proteins. A few of PriB proteins were published and...
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Study of radioluminescence in LiMgPO4 doped with Tb, B and Tm
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Amphotericin B and Its New Derivatives - Mode of Action
PublicationAmphotericin B (AmB) is a well known antifungal and antiprotozoal antibiotic used in the clinic for several decades. Clinicalapplications of AmB, however, are limited by its nephrotoxicity and many other acute side effects which are not acceptable by patientswhen their life is not threaten. In order to improve the therapeutic index of this drug, lipid formulations have been introduced and manyefforts have been made to obtain less...
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Ni2X2 (X = pnictide, chalcogenide, or B) based superconductors
PublicationPublikacja jest przeglądem właściwości nadprzewodników na bazie niklu, które zawierają płaszczyzny Ni2X2 (X=As, P, Bi, Si, Ge, B).
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Novel primosomal protein B from Clostridium pasteurianum
PublicationPriB is a primosomal protein that catalyzes DNA replication in Procaryota. The replication pathway starts with PriA protein - the initiator protein that binds to a DNA replication fork, unwinds double-stranded DNA and role of PriB is to stabilize PriA on the DNA. However there are many biochemical differences in replication mechanism in bacteria and only some of them use PriB proteins. A few of PriB proteins were published and...
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WEAR OF Si OR B DOPED AMORPHOUS CARBON COATINGS
PublicationThe paper describes a complex wear research on DLC (amorphous carbon) moped with boron (B) and silicone (Si). The tests were carried out in two different sliping systems: flat–on–flat (ring contact, unidirectional sliding) and ball–on–flat (reciprocating sliding). Water and medical saline solutions were used as lubricants. A comparative analysis of the results revealed differences in the initiation and progress of wear and the...
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Modyfikacje chemiczne Amfoterycyny B i Nystatyny A1
PublicationW ramach badań, opisanych w niniejszej rozprawie doktorskiej, przetestowano możliwości chemicznej modyfikacji części aminocukrowej aglikonu amfoterycyny B i nystatyny A1. Otrzymano chroniony aglikon AmB, posiadający grupę hydroksylową na atomie węgla C19, który posłużył jako substrat w reakcji substytucji nukleofilowej oraz dehydracyjnej glikozylacji. Opracowano i zoptymalizowano warunki syntezy chronionych pochodnych cukrowych,...
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Algorytmy numeryczne obliczania pseudokątów wiążących typu B
PublicationReferat tematycznie związany jest z teoretycznymi podstawami funkcjonowania technologii pomiarowej bazującej na stanowiskach swobodnie zorientowanych. Przedstawiono algorytmy obliczania pseudoobserwacji kątowych typu B (zwanych pseudokątami), wiążącymi sieć punktów odniesienia ze stanowiskami pomiarowymi. Pseudokąty wiążące typu B wykorzystuje się w sieciach obliczeniowych typu B.
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Rotating Magnetic Field Increases β-Lactam Antibiotic Susceptibility of Methicillin-Resistant Staphylococcus aureus Strains
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Preparation of bicyclic β-lactam and bicyclic 1,3- oxazinone scaffolds using combined cycloaddition and metathesis processes
PublicationA simple, efficient two-step method for the preparation of heterobicyclic compounds was developed. Starting from 5-acyl or 5-carbamoyl-2,2- dimethyl-1,3-dioxa-4,5-dione bicyclic scaffolds of 1-azabicyclo[5.2.0]non- 3-en-9-one, 6,9,10,10a-tetrahydro-4H-[1,3]oxazino[3,2-a]azepin-4-one, and 6,9,10,10a-tetrahydro-2H-[1,3]oxazino[3,2-a]azepine-2,4(3H)-dione were prepared using cycloaddition of thermally generated ketenes to aldimines...
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Photocatalytic activity of TiO2 polymorph B revisited: physical, redox, spectroscopic, and photochemical properties of TiO2(B)/anatase series of titanium dioxide materials
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N-(1-Piperidinepropionyl)amphotericin B methyl ester (PAME) - a new derivative of the antifungal antibiotic amphotericin B: Searching for the mechanism of its reduced
PublicationZ zastosowaniem techniki monowarstw Langmuira zbadano naturę oddziaływań pochodnej antybiotyku przeciwgrzybowego amfoterycyny B o obniżonej toksyczności tj. estru metylowego N-(1-piperydynopropionylo)amfoterycyny B (PAME) z komponentami błon biologicznych takich jak: ergosterol, cholesterol i modelowy fosfolipid DPPC i stwierdzono, że zróżnicowanie tych oddziaływań jest podstawą obniżonej toksyczności związku.
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Current molecular methods for the detection of hepatitis B virus quasispecies
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Molecular modelling of amphotericin B-ergosterol primary complex in water
PublicationBadano właściwości pierwotnego kompleksu amfoterycyny B z ergosterolem przy pomocy symulacji dynamiki molekularnej. Otrzymane w wyniku naszych symulacji rezultaty słabo odpowiadają postulowanym przez innych autorów modelom kompleksu antybiotyk-sterol. Z drugiej strony uzyskane geometrie nie są sprzeczne z wynikami eksperymentów biofizycznych dotyczących powstawania kompleksów w wodzie i w środowisku wodno-alkoholowym.
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Decreasing Vaccination Coverage Against Hepatitis B and Tuberculosis in Newborns
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Benign Acute Childhood Myositis During Influenza B Outbreak
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Narzędzia do kontroli jakości powietrza wewnętrznego / B. Zabiegała
PublicationPrzyjmuje się, że dorosły człowiek średnio 60% swojego życia spędza w domu, 30% w pracy, 5% w różnego rodzaju środkach transportu a tylko 3% na zewnątrz pomieszczeń. Powyższe liczby wskazują, że powietrze wewnętrzne może w istotny sposób oddziaływać na stan zdrowia i samopoczucie człowieka. Szeroko rozumiana kontrola jakości powietrza wewnętrznego jest więc niezbędnym elementem w zapewnieniu komfortu życia użytkownikom pomieszczeń...
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Efficient production of B-substituted single-wall carbon nanotubes
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