Search results for "DISCOVERY"
showing 10 items of 4119 documents
Near infrared dyes by combination of squaraine and ferrocene chromophores
2000
Abstract Squaraines represent a class of compounds which attracts a lot of attention in materials science. A synthetic sequence for the preparation of the symmetrical squaraines 12a , b , which contain ferrocene units as electron donors, is described. The compounds exhibit, in dichloromethane or chloroform, two intense absorption bands. One of them is located at 641/650 nm—a normal region for squaraines; however, the other band is strongly shifted to long wavelengths and has its maximum at 921/961 nm. Alkyl sidechains enhance the solubility of 12a , b , which represent a new type of NIR dyes.
High-Yield Formation of Arbutin from Hydroquinone by Cell-Suspension Cultures ofRauwolfia serpentina
1992
High-density cell-suspension cultures of Rauwolfia serpentina cultivated in a nutrition medium optimized for the production of the glucoalkaloid raucaffricine synthesize hydroquinone glycosides from continuously added hydroquinone with a total yield of 23.87 g/1 (18 g/1 of arbutin and 5.87 g/1 of a hydroquinone diglycoside) in 7 days. This arbutin production is by far the highest formation of a natural product by plant-cell-culture systems reported to date.
Interaction of pHPMA–pLMA Copolymers with Human Blood Serum and Its Components
2013
Immediately after administration, polymer therapeutics are exposed to complex biological media like blood which may influence and alter their physicochemical properties due to interactions with proteins or serum components. Among such interactions those leading to larger sized aggregates can be sensitively detected by dynamic light scattering (DLS) as a pre in vivo screening method. Random copolymers from N-(2-hydroxypropyl)methacrylamide and lauryl methacrylate p(HPMA-co-LMA) and copolymers loaded with the model drug domperidone were characterized by DLS in isotonic salt solution and in blood serum. The bare amphiphilic copolymer micelles (Rh=30 nm in isotonic salt solution) formed large a…
Characterisation of Diarylheptanoid- and Flavonoid-type Phenolics in Corylus avellana L. Leaves and Bark by HPLC/DAD-ESI/MS
2013
Introduction The leaves of Corylus avellana L. (common hazel, Betulaceae), a plant with a wide distribution in Europe, have been used in folk medicine for various diseases, but phytochemical exploration of C. avellana is still incomplete. To the best of our knowledge there is no previous report concerning diarylheptanoids in C. avellana, although these compounds show a frequent occurrence among Betulaceae plants. Objective To improve existing online chromatographic methods for the investigation of the phenolic compounds in C. avellana leaves and bark, focusing on diarylheptanoid-type molecules. Methods Dried and powdered leaves and bark of C. avellana were extracted with increasing polarity…
Structure and Photochemical Behavior of the Cyclodextrin Inclusion Complexes of the Benzoylthiophene-Derived Drugs Tiaprofenic Acid (=5-Benzoyl-α-met…
2001
The effect of β-cyclodextrin (β-CD) on the excited-state reactivity of the two benzoylthiophene derivatives, tiaprofenic acid (TPA; 2) and suprofen (SPF; 3) in their carboxylate forms is studied. The presence of β-cyclodextrin does not affect the nature of the photoproduced transients and the photoproducts, but increases the photodegradation quantum yields of both drugs. The efficiency of the photodecarboxylation process is enhanced. This effect is rationalized in the light of the inclusion of 2 and 3 in the β-CD cavity, affecting the energy of the lowest excited states of the drugs. The structure of the complexes is determined by induced circular dichroism, and molecular-mechanics and dyna…
Large Scale Synthesis of Mono- and Di-urethane Derivatives of Lysine.
1999
Orthogonally protected diurethane derivatives of lysine are valuable materials for peptide syntheses. An example is ZLys(Boc), which is exploited in the industrial production of certain well-established peptide drugs. 3,4) Another derivative is Fmoc-Lys(Boc), which is in common use in the laboratory synthesis of peptides. 5) The simplest route to these lysine derivatives seems to be using the copper complex for simultaneous protection of the a-amino and a-carboxyl function, N e -tert-butoxycarbonylation and then copper detachment. The obtained Lys(Boc) might be then subjected to N a -benzyloxycarbonylation.
Spectrophotometric determination of binding constants between some aminocyclodextrins and nitrobenzene derivatives at various pH values
2002
Abstract The inclusion capacity of three modified cyclodextrins—namely mono-(6- N , N -dimethylamino-6-deoxy)- ( 3 ), mono-6-(2-aminoethyl)-amino-6-deoxy- ( 4 ) and mono-6-(2- N , N -dimethylaminoethyl)-amino-6-deoxy- ( 5 ) β-cyclodextrin, with six para -substituted nitrobenzenes ( A – F ) has been investigated at three different pH values. Molecular interactions in inclusion complexes have also been investigated by means of molecular mechanics (MM2/QD) models. The desolvation of the cyclodextrin is the most important factor in determining the binding ability of the various hosts. However, for a given host, electrostatic and van der Waals interactions and the formation of a hydrogen bond be…
Binding equilibria between beta-cyclodextrin and p-nitro-aniline derivatives: the first systematic study in mixed water-methanol solvent systems.
2009
Abstract Complexation equilibria, in mixed water–methanol solvent media, between native β-cyclodextrin and a set of suitably selected p -nitro-aniline derivatives were studied by means of polarimetry. The effects exerted by the organic co-solvent on the conditional inclusion free energies Δ G cond 0 and the differential molar optical rotations Δ Θ were thoroughly analyzed under the perspective of the enthalpy–entropy compensation effect. Experimental data suggest an intimate participation (‘dynamic co-inclusion’) of solvent molecules in the formation and in the conformational dynamics of the host–guest inclusion complex.
Chiral recognition of protected amino acids by means of fluorescent binary complex pyrene/heptakis-(6-amino)-(6-deoxy)-β-cyclodextrin
2006
The ability of the binary complex pyrene (Py)/heptakis-(6-amino)-(6-deoxy)-β-cyclodextrin (am-β-CD) to act as a chiral selector was tested at two pH values (8.0 and 9.0). Phenylalanine (Phe), methionine (Met) and histidine (His) were used as chiral model molecules. The stability of ternary complexes Py/am-β-CD/amino acid was determined by means of spectrofluorimetric measurements. The data collected showed an increase in stability going from the binary to ternary complex and above all the possibility to use the binary complex as a chiral selector. Finally, data collected at two pH values showed that the binary complex is a better chiral selector when charged rather than in its neutral form.
Binding properties of mono-(6-deoxy-6-amino)-β-cyclodextrin towards p-nitroaniline derivatives: a polarimetric study
2009
Abstract Polarimetry was used in order to investigate the formation of supramolecular complexes between mono-6-amino-β-cyclodextrin and various p-nitroaniline derivatives at two different pH values. Comparison with the behaviour of native β-cyclodextrin gave us the opportunity to consider the effect exerted by the presence of charged groups, having different solvation requirements, on the binding equilibrium. Data offer some support to the hypothesis of ‘dynamic co-inclusion’ of solvent molecules within the host–guest complex.