- The discovery and enhanced properties of trichain lipids in lipopolyplex gene delivery systems
-
The formation of a novel trichain (TC) lipid was discovered when a cationic lipid possessing a terminal hydroxyl group and the helper lipid dioleoyl l-α-phosphatidylethanolamine (DOPE) were formulated as vesicles and stored. Importantly, the transfection efficacies of lipopolyplexes comprised of the TC lipid, a targeting peptide and DNA (LPDs) were found to be higher than when the corresponding dichain (DC) lipid was used. To explore this interesting discovery and determine if this concept can be more generally applied to improve gene delivery efficiencies, the design and synthesis of a series of novel TC cationic lipids and the corresponding DC lipids was undertaken. Transfection efficacies of the LPDs were found to be higher when using the TC lipids compared to the DC analogues, so experiments were carried out to investigate the reasons for this enhancement. Sizing experiments and transmission electron microscopy indicated that there were no major differences in the size and shape of the LPDs prepared using the TC and DC lipids, while circular dichroism spectroscopy showed that the presence of the third acyl chain did not influence the conformation of the DNA within the LPD. In contrast, small angle neutron scattering studies showed a considerable re-arrangement of lipid conformation upon formulation as LPDs, particularly of the TC lipids, while gel electrophoresis studies revealed that the use of a TC lipid in the LPD formulation resulted in enhanced DNA protection properties. Thus, the major enhancement in transfection performance of these novel TC lipids can be attributed to their ability to protect and subsequently release DNA. Importantly, the TC lipids described here highlight a valuable structural template for the generation of gene delivery vectors, based on the use of lipids with three hydrophobic chains.
- Mohammadi, Atefeh,Kudsiova, Laila,Mustapa, M. Firouz Mohd,Campbell, Frederick,Vlaho, Danielle,Welser, Katharina,Story, Harriet,Tagalakis, Aristides D.,Hart, Stephen L.,Barlow, David J.,Tabor, Alethea B.,Lawrence, M. Jayne,Hailes, Helen C.
-
-
Read Online
- Surface-promoted aggregation of amphiphilic quadruplex ligands drives their selectivity for alternative DNA structures
-
Scientists are currently truly committed to enhance the specificity of chemotherapeutics that target DNA. To this end, sequence-specific drugs have progressively given way to structure-specific therapeutics. However, while numerous strategies have been implemented to design high-affinity candidates, strategies devoted to the design of high-selectivity ligands are still rare. Here we report on such an approach via the study of an amphiphilic compound, TEGPy, that self-assembles at a liquid/solid interface to provide nanosized objects that are stable in water. The resulting aggregates, identified through atomic force microscopy measurements, were found to disassemble upon interaction with DNA in a structure-specific manner (quadruplex- versus duplex-DNA). Our results provide a fertile ground for devising new strategies aiming at concomitantly enhancing DNA structural specificity and the water-solubility of aggregation-prone ligands. This journal is
- Laguerre, Aurélien,Chang, Yi,Pirrotta, Marc,Desbois, Nicolas,Gros, Claude P.,Lesniewska, Eric,Monchaud, David
-
-
Read Online
- triAZOLOtriAZINE DERIVATIVES AS A2A RECEPTOR ANTAGONISTS
-
The present invention provides triazolotriazine derivatives of formula (1) as A2A receptor antagonists. Compounds of formula (1) and pharmaceutical compositions including the compounds can be used for the treatment of disorders related to A2A receptor hyperfunctioning, such as certain types cancers. Compounds of formula (1) and methods of preparing the compounds are disclosed in the invention.
- -
-
Page/Page column 38-39
(2020/01/24)
-
- Synthesis of Phosphonic Acid Ligands for Nanocrystal Surface Functionalization and Solution Processed Memristors
-
Here, we synthesized 2-ethylhexyl, 2-hexyldecyl, 2-[2-(2-methoxyethoxy)ethoxy]ethyl, oleyl, and n-octadecyl phosphonic acid and used them to functionalize CdSe and HfO2 nanocrystals. In contrast to branched carboxylic acids, postsynthetic surface functionalization of CdSe and HfO2 nanocrystals was readily achieved with branched phosphonic acids. Phosphonic acid capped HfO2 nanocrystals were subsequently evaluated as memristors using conductive atomic force microscopy. We found that 2-ethylhexyl phosphonic acid is a superior ligand, combining a high colloidal stability with a compact ligand shell that results in a record-low operating voltage that is promising for application in flexible electronics.
- De Roo, Jonathan,Zhou, Zimu,Wang, Jiaying,Deblock, Loren,Crosby, Alfred J.,Owen, Jonathan S.,Nonnenmann, Stephen S.
-
p. 8034 - 8039
(2018/10/25)
-
- Quaternary ammonium salt functionalized spherical conjugated polymer nanoparticle and antibacterial application thereof
-
The invention discloses a quaternary ammonium salt functionalized spherical conjugated polymer nanoparticle and antibacterial application thereof. The nanoparticle takes hydrophobic conjugated polymeras an inner core; a quaternary ammonium salt functional group molecule forms a housing on the surface through the hydrophobic effect, so that the spherical conjugated polymer nanoparticle is finallyobtained; the structural formula of the hydrophobic conjugated polymer is FORMULA as shown in the description; and the structural formula of the quaternary ammonium salt functional group molecule is FORMULA as shown in the description. Under a light-shielding condition, the conjugated polymer nanoparticle can realize broad-spectrum efficient bacteria resistance without a light source or other energy, has an antibacterial rate which is far higher than that of functional group molecule of the same concentration, is not liable to generate drug resistance, and provides a novel idea for developingan antibacterial nano material in the future.
- -
-
-
- Glycol-functionalized ionic liquids for high-temperature enzymatic ring-opening polymerization
-
Enzymatic ring-opening polymerization (ROP) is a benign method for preparing polyesters, such as polylactides and other polylactones. These reactions are typically carried out at relatively high temperatures (60-130 °C), however, there is a deficiency of enzyme-compatible solvents for such thermally-demanding biocatalytic processes. In this study, we have prepared a series of short-chained glycol-grafted ionic liquids (ILs) based on a phosphonium, imidazolium, pyridinium, ammonium, or piperidinium cationic headgroup. Most of these glycol-grafted ILs exhibit relatively low dynamic viscosities (33-123 mPa s at 30 °C), coupled with excellent short-term thermal stabilities with decomposition temperatures (Tdcp) in the 318-403 °C range. Significantly, the long-term thermal stability under conditions matching those for enzymatic ROP synthesis (130 °C for 7 days) is excellent for several of these task-specific ILs. Using Novozym 435-catalyzed ROP, these ILs are demonstrated to be viable solvents for the enzymatic production of reasonable yields (30-48%) of high molecular mass (Mw ~20 kDa) poly(l-lactide) and poly(?-caprolactone) compared to solventless conditions (12-14 kDa).
- Zhao, Hua,Afriyie, Lennox O.,Larm, Nathaniel E.,Baker, Gary A.
-
p. 36025 - 36033
(2018/11/20)
-
- Polyethylene glycol derivatization of the non-active ion in active pharmaceutical ingredient ionic liquids enhances transdermal delivery
-
We report the synthesis of four salts composed of the salicylate anion ([Sal]?) paired with tributylammonium ([HN444]+), choline ([Cho]+), 1-methylpyrrolidinium ([HMPyrr]+), and triethylene glycol monomethyl ether tributylammonium ([mPEG3N444]+) cations. Three of the synthesized salts (room temperature liquids [mPEG3N444][Sal] and [Cho][Sal], and a supercooled liquid [HN444][Sal]) belong to the category of ionic liquids (ILs), and one salt (solid [HMPyrr][Sal]) was a crystalline solid. ILs in their neat form were studied for membrane transport through a silicon membrane, and exhibited higher transport compared to a control experiment with sodium salicylate dissolved in mPEG3OH as solvent, but lower membrane transport compared to salicylic acid dissolved in mPEG3OH. The ‘PEGylated’ IL, [mPEG3N444][Sal], crossed the membrane with an ca. ~2.5-fold faster rate than that of any of the non-PEGylated ILs. This work demonstrates not only that API-ILs can eliminate the use of a solvent vehicle during application and notably transport through a membrane as opposed to a higher melting crystalline salt, but also that the membrane transport can be further enhanced by PEGylation of the counter ions.
- Zavgorodnya, Oleksandra,Shamshina, Julia L.,Mittenthal, Max,McCrary, Parker D.,Rachiero, Giovanni P.,Titi, Hatem M.,Rogers, Robin D.
-
p. 1499 - 1508
(2017/02/23)
-
- Construction and luminescence property of a highly ordered 2D self-assembled amphiphilic bidentate organoplatinum(II) complex
-
Rod-coil shaped amphiphilic bidentate dichloro(phenanthroline)platinum(ii) complexes, 1-Pt and 2-Pt, which possess different hydrophilic lateral chains on one side of an identical aromatic rod core, are synthesized. 1-Pt first forms dimers then arranges into well-defined two-dimensional (2D) films consisting of highly ordered molecular arrays both from methanol and on substrate. 2-Pt, as a building-block, yields micrometer-sized rigid 2D sheets without formation of an initial dimer. Red luminescence of the film is induced by self-assembly of nonemissive 1-Pt molecules, whereas sheets based on nonemissive 2-Pt gives weak yellow emission. These results indicate that the coil-rod ratio plays an important role in the structure and optical properties of these self-assemblies. Moreover, the film on the substrate at the macroscopic scale, exhibits multi-stimuli responsiveness, which predicts its application in smart chemosensing devices and probes.
- Xiang, Yunjie,Li, Wenjing,Fang, Yuxi,Zhang, Dengqing,Li, Xianying,Jin, Wusong
-
p. 27360 - 27369
(2016/03/30)
-
- Preparation method of non-ionic fullerene-containing amphiphilic molecule
-
The invention relates to a preparation method of a non-ionic fullerene-containing amphiphilic molecule. According to the invention, oligomeric ethylene glycol monomethyl ether bromo-derivative and hydroxy benzene (naphthalene, pyrene) formaldehyde are used as raw materials to synthesize an intermediate product oligomeric ethylene glycol monomethyl ether substituted benzene (naphthalene, pyrene) formaldehyde; and then, oligomeric ethylene glycol monomethyl ether substituted benzene (naphthalene, pyrene) formaldehyde is used as a donor unit and fullerene is used as a receptor so as to synthesize the non-ionic fullerene-containing amphiphilic molecule. The target product obtained has advantages of novel structure, high heat stability and adjustable solubility, can form a self-assembly structure in a solution and under the solvent-free condition, and is suitable for fields of surface chemistry, supramolecular self-assembly, photoelectronic device and the like.
- -
-
Paragraph 0052
(2017/02/02)
-
- Self-Organization and Vesicle Formation of Amphiphilic Fulleromonodendrons Bearing Oligo(poly(ethylene oxide)) Chains
-
A new series of N-methylfulleropyrrolidines bearing oligo(poly(ethylene oxide))-appended Percec monodendrons (fulleromonodendrons, 4a-f) have been synthesized. The substituted position of the oligo(poly(ethylene oxide)) chain(s) on the phenyl group of the Percec monodendron for 4a-f was varied, which is at the 4-, 2,4-, 3,5-, 3,4,5-, 2,3,4- and 2,4,6- position, respectively. 4a-e are obtained as solids at 25°C and can self-organize into lamellar phases as revealed by X-ray diffraction (XRD) and small-angle X-ray scattering (SAXS) measurements, while 4f appears as a viscous liquid. The substitution patterns of the oligo(poly(ethylene oxide)) chain(s) also significantly influence the solubility of 4a-f, especially in ethanol and water. Formation of self-organized supramolecular structures of 4d and 4e in water as well as 4d in ethanol is evidenced from UV-vis and dynamic light scattering (DLS) measurements. Further studies in water using various imaging techniques including transmission electron microscopy (TEM), freeze-fracture TEM (FF-TEM), cryo-TEM and atomic force microscopy (AFM) observations revealed the formation of well-defined vesicles for 4d and plate-like aggregates for 4e, indicating that the aggregation behavior of the fulleromonodendrons is highly dependent on their molecular structures. For 4d in ethanol, only irregular aggregates were noticed, indicating the solvent also plays a role on regulating the aggregation behavior. After functionalization with the Percec monodendrons, 4a-f can preserve the intriguing electrochemical properties of pristine C60 as revealed by cyclic voltammetries. The thermotropic properties of 4a-f have also been investigated. It was found that all of them show good thermal stability, but no mesophases were detected within the investigated temperature ranges. (Figure Presented).
- Chen, Mengjun,Zhu, Hongxia,Zhou, Shengju,Xu, Wenlong,Dong, Shuli,Li, Hongguang,Hao, Jingcheng
-
p. 2338 - 2347
(2016/03/26)
-
- Compounds with higher PKG (protein kinase G) inhibitory activity and preparation method of compounds
-
The invention discloses compounds which have higher PKG (protein kinase G) inhibitory activity and are represented as a formula I, pharmaceutically acceptable salts, pharmaceutical composition containing the novel compounds, as well as an application of the novel compounds in treatment of pain, especially chronic pain. The invention further discloses a preparation method of the compounds and new intermediates. R1 and R2 are the same or different and are selected from a group comprising halogen (such as F or Cl), C1-C6 alkoxy, C1-C6 alkyl, C2-C6 alkenyl and C2-C6 alkynyl; R3 is a terminal group and is selected from a group comprising H, halogen, alkyl, naphthenic base, alkenyl, alkynyl, aryl and heteroaryl; n is the number of repetitive units and is an integer in a range from 1 to 15.
- -
-
-
- COMPOUND HAVING HIGHER INHIBITION OF PROTEIN KINASE G ACTIVITY AND PREPARATION METHOD THEREFOR
-
Disclosed are a compound of Formula I having higher inhibition of protein kinase G (PKG) activity and pharmaceutically acceptable salts thereof. In Formula I, R1 and R2 are the same or different, each being independently chosen from the halogens, the C1-C6 alkoxyl group, the C1-C6 alkyl group, the C2-C6 alkenyl group, and the C2-C6 alkynyl group; R3 is chosen from H, the halogens, the substituted or unsubstituted C1-C6 alkyl group, C3-C6 cycloalkyl group, C2-C6 alkenyl group, and C2-C6 alkynyl group, aryl group, and heteroaryl group; and n is an integer between 0 and 15. Also disclosed is a pharmaceutical composition comprising said compound, the use of the compound in treating pains, in particular chronic pain, a preparation method for the compound, and a new intermediate.
- -
-
-
- A highly water-dispersible/magnetically separable palladium catalyst based on a Fe3O4@SiO2 anchored TEG-imidazolium ionic liquid for the Suzuki-Miyaura coupling reaction in water
-
A novel ionic liquid functionalized magnetic nanoparticle was prepared by anchoring an imidazolium ionic liquid bearing triethylene glycol moieties on the surface of silica-coated iron oxide nanoparticles. The material proved to be an effective host for the immobilization of a Pd catalyst through a subsequent simple ion-exchange process giving a highly water dispersible, active and yet magnetically recoverable Pd catalyst (Mag-IL-Pd) in the Suzuki-Miyaura coupling reaction in water. The as-prepared catalyst displayed remarkable activity toward challenging substrates such as heteroaryl halides and ortho-substituted aryl halides as well as aryl chlorides using very low Pd loading in excellent yields and demonstrating high TONs. Since the catalyst exhibited extremely low solubility in organic solvent, the recovered aqueous phase containing the catalyst can be simply and efficiently used in ten consecutive runs without significant decrease in activity and at the end of the process can be easily separated from the aqueous phase by applying an external magnetic field. This novel double-separation strategy with negligible leaching makes Mag-IL-Pd an eco-friendly and economical catalyst to perform this transformation. the Partner Organisations 2014.
- Karimi, Babak,Mansouri, Fariborz,Vali, Hojatollah
-
p. 2587 - 2596
(2014/05/06)
-
- NOVEL COMPOSITIONS AND METHODS FOR TREATING CANCER
-
Provided herein are methods and compositions inter alia for treating diseases, including hyperproliferative diseases, migraine headaches, and depression.
- -
-
Paragraph 0491-0492
(2013/05/21)
-
- Toward stable electron paramagnetic resonance oximetry probes: Synthesis, characterization, and metabolic evaluation of new ester derivatives of a tris-(para-carboxyltetrathiaaryl)methyl (TAM) radical
-
Tris(p-carboxyltetrathiaaryl)methyl (TAM) radicals, such as 1a ("Finland" radical), are useful EPR probes for oximetry. However, they are rapidly metabolized by liver microsomes in the presence of NADPH, with the formation of diamagnetic quinone-methide metabolites resulting from an oxidative decarboxylation of one of their carboxylate substituents. In an effort to obtain TAM derivatives potentially more metabolically stable in vivo, we have synthesized four new TAM radicals in which the carboxylate substituents of 1a have been replaced with esters groups bearing various alkyl chains designed to render them water-soluble. The new compounds were completely characterized by UV-vis and EPR spectroscopies, high resolution mass spectrometry (HRMS), and electrochemistry. Two of them were water-soluble enough to undergo detailed microsomal metabolic studies in comparison with 1a. They were found to be stable in the presence of the esterases present in rat liver microsomes and cytosol, and, contrary to 1a, stable to oxidation in the presence of NADPH-supplemented microsomes. A careful study of their possible microsomal reduction under anaerobic or aerobic conditions showed that they were more easily reduced than 1a, in agreement with their higher reduction potentials. They were reduced into the corresponding anions not only under anaerobic conditions but also in the presence of dioxygen. These anions were much more stable than that of 1a and could be characterized by UV-vis spectroscopy, MS, and at the level of their protonated product. However, they were oxidized by O2, giving back to the starting ester radicals and catalyzing a futile cycle of O2 reduction. Such reactions should be considered in the design of future stable EPR probes for oximetry in vivo.
- Decroos, Christophe,Balland, Véronique,Boucher, Jean-Luc,Bertho, Gildas,Xu-Li, Yun,Mansuy, Daniel
-
p. 1561 - 1569
(2013/11/19)
-
- OPHTHALMIC COMPOSITIONS
-
The present invention relates to compositions that may alleviate symptoms of ocular stress, as well as methods of their production, use, and storage compositions. The compositions comprise at least one ocular epithelial cell associating group and at least one hydrophilic group. In one embodiment the at least one ocular epithelial cell associating group and at least one hydrophilic group are substituents on a conjugated polyaromatic core. The compositions may be used in ophthalmic compositions and ophthalmic devices.
- -
-
-
- A novel water-soluble NHC-Pd polymer: An efficient and recyclable catalyst for the Suzuki coupling of aryl chlorides in water at room temperature
-
A novel water-soluble NHC-Pd polymer with triethylene glycol legs was developed as a water soluble and highly recyclable catalyst that shows high catalytic activity in the Suzuki-Miyaura coupling of aryl chlorides in high yields in water at room temperature.
- Karimi, Babak,Fadavi Akhavan, Pari
-
supporting information; experimental part
p. 7686 - 7688
(2011/09/12)
-
- Europium complexes of tris(dipicolinato) derivatives coupled to methylumbelliferone: A double sensitization
-
A para-poly(oxyethylene) dlpicolinic acid, derivative coupled to methylumbelliferone was synthesized and used, as a ligand for coordination with europium ions. Characterization of the complex by mass spectrometry and spectrophotometry was performed in aqueous solution and points to the formation of the 1:3 Eu/L complex. Physicochemlcal properties are close to those of already reported dipicolinato complexes, confirming that the presence of a coumarin chromophore does not interfere with complex formation. Photophysical measurements result in observed, lifetimes of 1.4 ms and intrinsic quantum, yields, ΦEuEu, ranging from 33 to 50% (depending on the solvent used). Selective excitation can be performedeither mostly on the dipicolinate (DPA) backbone (at 280 nm) or exclusively on the coupled coumarin chromophore in the near visible range (320 nm). Despite the spatial distance between the antenna and the lanthanide ion, europium emission was observed upon 320 nm excitation together with the coumarin emission. The different sensitization pathways have been explored and rationalized. Finally, the complex has been used to probe the ratio of a binary mixture of solvent, establishing the potential interest of this new class of ligands in many fields of research, from photophysics to applied chemistry.
- Andres, Julien,Chauvin, Anne-Sophie
-
experimental part
p. 2700 - 2713
(2010/08/21)
-
- NOVEL POLYBENZOFULVENE DERIVATIVES, SYNTHESIS AND USES THEREOF
-
The present invention relates to polymers of formula poly-3 (I), their synthesis, intermediates and uses thereof.
- -
-
Page/Page column 18-19
(2010/11/30)
-
- Synthesis of hydrophilic Fischer carbene complexes as organometallic marker and PEGylating agent for proteins
-
Syntheses of Fischer carbene complexes with various hydrophilic tethers (4, 6a, 6b, 6c, 8a, 8b, 14a, 14b, 15 and 19) are described. The water-soluble carbene complex, 14b, was used to label and pegylate bovine serum albumin (BSA) without affecting its conformation. The red complex, 19, underwent a sharp color change to yellow on reaction with BSA, a feature that is potentially useful for developing assay methods.
- Samanta, Debasis,Sawoo, Sudeshna,Patra, Subrata,Ray, Manju,Salmain, Michèle,Sarkar, Amitabha
-
p. 5581 - 5590
(2007/10/03)
-
- Synthesis of diindolocarbazoles by Ullmann reaction: A rapid route to ladder oligo(p-aniline)s
-
(Chemical Equation Presented) New and facile synthesis of symmetric diindolocarbazoles was developed using the copper-catalyzed Ullmann reaction. The key step is a double-intramolecular cyclization reaction realized on N-alkyl-3,6-dibromo-2,7-bis(2′aminophenyl)carbazole derivatives which offers the desired symmetric ladder oligo(p-aniline)s. Depending upon the nature of the side- and/or end-groups, well-defined thin films and/or semiladder polymers could be obtained. These electroactive ladder oligomers may have great potential in organic electronics.
- Wakim, Salem,Bouchard, Jimmy,Blouin, Nicolas,Michaud, Alexandre,Leclerc, Mario
-
p. 3413 - 3416
(2007/10/03)
-
- Synthesis and characterization of novel tetra- and octa-triethyleneoxysulfanyl substituted phthalocyanines forming lyotropic mesophases
-
Metal-free phthalocyanines and nickel phthalocyanines carrying four or eight oligo(ethyleneoxy)thia groups of peripheral positions have been synthesized from new phthalonitrile derivatives. These phthalocyanine derivatives were characterized both thermotropic and lyotropic mesophases by DSC and X-ray.
- Dabak, Salih,Ahsen, Vefa,Heinemann, Frauke,Zugenmaier, Peter
-
p. 111 - 127
(2007/10/03)
-
- Synthesis and properties of low-bandgap zwitterionic and planar conjugated pyrrole-derived polymeric sensors. Reversible optical absorption maxima from the UV on the near-IR
-
Described are the polymerizations of three new dibrominated carbonyl-stabilized ylide monomers using copper-bronze in DME to afford polymers that are soluble in common solvents and have unique optical and electronic properties. The first monomer is a zwitterionic N-butylpyrrolinium oxide derivative which, upon polymerization, gives a polymer that has a strong optical absorbance at 520 nm in CCl4. An interunit ionic interaction is proposed to explain this large red-shifted band. Bronsted bases and Lewis bases induce a reversible structural change in the polymer to give bathochromic shifts from the visible to the near-IR spectral region. Upon mild reduction of the zwitterionic polymer with Pd/C and H2 (1 atm), some of the extended conjugation is lost, but a polymer forms that has an enormous optical absorption maximum range from the near-LV (290 nm) to the near-IR (886 nm) depending on the solvent or hydroxide concentration. A sample of the reduced polymer can be dispersed in platicized poly(vinyl chloride). The flexible polymer composite reversibly changes from dark blue-brown in aqueous sodium hydroxide to bright yellow-orange in aqueous HCl. The second monomer, a zwitterionic N-dodecylpyrrolinium oxide derivative, was also synthesized in three steps from pyrrole and, upon polymerization, gives rise to a polymer which also responds reversibly toward Bronsted and Lewis bases. This polymer can be solution cast into flexible free-standing films. The third monomer is a zwitterionic N-[oligo(ethylene glycol) monomethyl ether]pyrrolinium oxide derivative which, upon polymerization, affords a polymer that not only responds reversibly toward Bronsted and Lewis bases but also is water soluble and optically sensitive toward the addition of specific salts. The presence of the oligoethylene substituents is critical for the dramatic ionochromic response. Additionally, Pd-catalyzed cross-coupling methodology can be used for the incorporation of the N-butylpyrrolinium oxide monomer unit into an AB-type oligomeric system where the B component is a 1,4-phenylene moiety.
- Brockmann,Tour
-
p. 4437 - 4447
(2007/10/02)
-
- Platinum(II) complexes, their preparation and use as anti-tumor agents
-
Compounds of formula I STR1 wherein R1 and R2, that can be the same or different, are hydrogen, alkyl, aryl, aralkyl groups or, if taken together, cycloalkyl groups; A is a carbon atom, a residue of 2,3-dioxybutandioic-2,4-dioxyphtalic acid or disubstituted malonic acid derivatives; n1 and n2 are selected in such a manner that the result of their addition is from 2 to 40; T1 and T2 that can be the same or different, are hydrogen, alkyl, benzyl, phenyl, acyl or cycloalkyl or a residue of formulae STR2 Compounds I are useful as anti-tumor agents in human therapy.
- -
-
-
- 2-sulphinyl-acetyl-1,3-thiazolidines, their preparation and pharmaceutical compositions
-
Thiazolidines of formula I STR1 wherein R is H, C1 -C4 -alkyl, allyl or propargyl; X is O, CH2, S; R1 is C1 -C6 -linear or branched alkyl, phenyl, benzyl, or a group of formula CH2 --CH2 --O--(CH2 --CH2 --O)n --Ra wherein n is zero or an integer from 1 to 3 and Ra is H, benzyl or C1 -C6 -linear or branched alkyl. Compounds I are endowed with favourable therapeutical properties for pathologies of the respiratory system.
- -
-
-
- 2-Sulphinyl-acetyl-1,3-thiazolidines, their preparation and pharmaceutical compositions
-
Thiazolidines of formula I - wherein R is H, C1-C4-alkyl, allyl or propargyl;, - X is O, CH2, S;, - R1 is C1-C6-linear or branched alkyl, phenyl, benzyl, or a group of formula CH2-CH2-O-(CH2-CH2-O)n-Ra, wherein n is zero or an integer from 1 to 3 and Ra is H, benzyl or C1-C6-linear or branched alkyl. Compounds I are endowed with favourable therapeuti-cal properties for pathologies of the respiratory system.
- -
-
-
- Preparation of 6,9,12-Trioxatridecylmethylsilyl Substituted Silica, a New Stationary Phase for Liquid Chromatography
-
The preparation of a substituted silica containing chemically inert ether groups is described, together with the synthesis of the derivative used for the substitution.The material shows excellent wetting properties in water containing solvent mixtures, and the utility as stationary phase for the chromatographic purifying of a partly protected decapeptide is shown.
- Schou, Ole,Larsen, Per
-
p. 337 - 340
(2007/10/02)
-