- Cascade Polymers: Syntheses and Characterization of One-Directional Arborols Based on Adamantane
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Several methods for the synthesis of cascade polymers (dendritic macromolecules) on adamantane have been investigated.The synthesis of two novel, branched monomers, 4-amino-4-(3-acetoxypropyl)-1,7-diacetoxyheptane and di-tert-butyl 4-amino-4-heptanedioate, possessing 3-fold symmetry and branches emanating from a tetrahedral carbon branch point, is described.These monomers were reacted with a mono-functional adamantane core to evaluate the reaction efficiency, ease of purification of products, and spectral characteristics.
- Newkome, George R.,Behera, Rajani, K.,Moorefield Charles N.,Baker, Gregory, R.
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- Generation effect of Newkome dendrimers on cellular uptake
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Poly(amide)-based dendrimers can be used as delivery scaffolds in conjunction with the cell-penetrating peptide gH625 derived from the glycoprotein of the Herpes Simplex virus type 1. In this contribution, we aim to isolate the optimal dendrimer generation for cellular uptake for Newkome type dendrimers conjugated with gH625. For this study, we synthesized generations zero to three of the Newkome dendrimer-gH625 bioconjugate. Fluorescent microscopy experiments showed that the second and third generations are the most efficient for cellular uptake with the second generation having the synthetic advantage. The optimal second generation can be used as an improved material for a dendrimer based delivery scaffold for peptide therapeutics.
- Kaufman, Elizabeth A.,Tarallo, Rossella,Falanga, Annarita,Galdiero, Stefania,Weck, Marcus
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- Synthesis, characterization and computational modeling of cyclen substituted with dendrimeric branches. Dendrimeric and macrocyclic moieties working together in a collective fashion
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A molecular system, formed by the aza-macrocycle known as cyclen and functionalized dendrons, was synthesized in a convergent fashion. An aliphatic spacer between the two molecular units was incorporated to avoid the sterical hindrances. The N-acylation reactions to carry out the cyclen substitution, particularly those in solid state, resulted in very good yields since no further purifications were necessary. The obtained molecular system was characterized by common spectroscopic techniques. According to X-ray analysis (powder analysis), there is a random arrangement of the molecules, with an average interplanar distance (the most recurrent) of 4.8 ? between first neighbors. A theoretical study at DFT level of theory was carried out, simulating the inclusion process of Ni2+ into two different model molecules (A and C), with and without dendrons present. According to the calculated interaction energies in the inclusion process, there is a significant contribution in terms of energy (-60.89 Kcal/mol) due to the presence of functionalized dendrons, which enfold the metal ion, forming a molecular cage and increasing in this way the degree of pre-organization due to cooperative effects created by the dendrimeric environment. These molecular arrangements would be relevant in areas like catalysis, having influence on the selectivity of catalytic processes, by controlling the accessibility of the active site (the metal atom) via sterical hindrances. Further experimental work of the incorporation of metal ions of the first transition series will be done in a rational way, taking into account the theoretical results obtained so far.
- Cruz-Morales, Jorge A.,Guadarrama, Patricia
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- Synthesis and spectroscopic characterization of a new tripodal hexadentate iron chelator incorporating catechol units
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We report the synthesis and physicochemical properties of a new tripodal hexadentate chelator (catTHC) synthesized by reaction of a flexible tripodal backbone with three bidentate catechol units. To improve the efficiency of the amide coupling reaction, classical conditions using two pairs of coupling reactants were tested, and a significant reduction in reaction time was achieved by using microwave irradiation with the reactants DCC/HOBt. Subsequent removal of the benzyl protecting groups using BCl3 in dichloromethane provided the final chelator in good yield. The acid-base properties of catTHC in aqueous solution and the affinity of the ligand towards iron(III) were investigated at variable pH and in the presence of iron(III) using spectroscopic methods. The hexadentate ligand forms a 1:1 complex with iron(III) whose stability constant was determined by competition with EDTA. The values obtained for the stability constant and pFe3+ are log β110 = 36.70 and pFe3+ = 26.7.
- Queirós, Carla,Leite, Andreia,Silva, Ana M.G.,Gameiro, Paula,De Castro, Baltazar,Rangel, Maria
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- Rapid method for reducing nitro in aliphatic nitro compound into amino
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The invention discloses a rapid method for reducing nitro in an aliphatic nitro compound into amino. According to the method, raney nickel is adopted as a catalyst, hydrazine hydrate is adopted as a reducing agent, ethyl alcohol or methyl alcohol is adopted as a solvent, reaction is carried out at the reaction temperature of 60-70 DEG C, the reaction for reducing a whole aliphatic nitro compound into an aliphatic amino compound can be completed very quickly, and the reaction time does not exceed 2 hours. The method has the advantages of rapid reaction, no need of pressurization or sealing, noneed of inert gas protection, high yield and suitability for mass production.
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Paragraph 0027-0029
(2020/07/13)
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- Multifunctional degradable nanoparticles with control over size and functionalities
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In one aspect, the invention relates to polymers, crosslinked polymers, functionalized polymers, nanoparticles, and functionalized nanoparticles and methods of making and using same. In one aspect, the invention relates to degradable polymers and degradable nanoparticles. In one aspect, the invention relates to methods of preparing degradable nanoparticles and, more specifically, methods of controlling particle size during the preparation of degradable nanoparticles. In one aspect, the degradable nanoparticles are useful for complexing, delivering, and releasing payloads, including pharmaceutically active payloads. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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Page/Page column 128
(2018/02/03)
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- Multi-branched triazine derivative and application of same
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The invention relates to a multi-branched 1,3,5-triazine derivative and an application thereof. In the invention, a multi-branched amphiphilic molecule, which is easy to prepare and is higher than 30% in total yield, is designed since a symtriazine ring is not damaged due to tolerance against various severe reaction conditions and the three chlorine atoms on a cyanuric chloride ring have unique reaction features; the multi-branched amphiphilic molecule not only can be used as a surfactant independently, but also can be combined with other cationic surfactants.
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Paragraph 0043-0044; 0046
(2018/03/28)
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- Platform Synthetic Lectins for Divalent Carbohydrate Recognition in Water
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Biomimetic carbohydrate receptors (“synthetic lectins”) have potential as agents for biological research and medicine. However, although effective strategies are available for “all-equatorial” carbohydrates (glucose, etc.), the recognition of other types of saccharide under natural (aqueous) conditions is less well developed. Herein we report a new approach based on a pyrene platform with polar arches extending from aryl substituents. The receptors are compatible with axially substituted carbohydrates, and also feature two identical binding sites, thus mimicking the multivalency observed for natural lectins. A variant with negative charges forms 1:2 host/guest complexes with aminosugars, with K1>3000 m?1for axially substituted mannosamine, whereas a positively charged version binds the important α-sialyl unit with K1≈1300 m?1.
- Carter, Tom S.,Mooibroek, Tiddo J.,Stewart, Patrick F. N.,Crump, Matthew P.,Galan, M. Carmen,Davis, Anthony P.
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p. 9311 - 9315
(2016/08/05)
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- CONJUGATES AND THEIR USES IN MOLECULAR IMAGING
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The present invention relates to bifunctional compounds, the bifunctional compounds for use in molecular imaging and therapy, methods of molecular imaging using the bifunctional compounds and kits including the bifunctional compounds for use molecular imaging. The bifunctional compounds have a tripodal hydroxypyridinone chelating portion and may be conjugated to a targeting group so that the compounds target specific cells or tissues in a subject.
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- SACCHARIDE CONJUGATES
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This invention relates to compounds comprising a saccharide conjugated to an imaging agent or a reporter group, compositions comprising them and methods of using them. Specifically BLM-disaccharide and BLM-monosaccharide conjugates containing different linker groups and an imaging agent or a reporter group are provided for the targeting and imaging of tumors.
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- SUGAR-LINKER-DRUG CONJUGATES
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The present disclosure relates to sugar-linker-drug conjugates, of the formula [A-B-]n-L-D, wherein A is a saccharide; B is a spacer, n is an integer selected from 1 to 3; L is a linker group and D is a drug having a chemically reactive functional group selected from the group consisting of a primary or secondary amine, hydroxyl, sulfhydryl, carboxyl, aldehyde and ketone. Pharmaceutical compositions comprising the conjugates and methods of using thern are also provided.
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Paragraph 0314
(2014/09/29)
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- GLYCOPEPTIDE AND LIPOGLYCOPEPTIDE ANTIBIOTICS WITH IMPROVED SOLUBILITY
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The invention relates to derivatives of glycopeptide and lipoglycopeptide antibiotics possessing an altered ionization state with respect to the parent glycopeptide or lipoglycopeptide antibiotic, and having the ability to be regenerated as the parent gly
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- Efficient bifunctional gallium-68 chelators for positron emission tomography: Tris(hydroxypyridinone) ligands
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A new tripodal tris(hydroxypyridinone) bifunctional chelator for gallium allows easy production of 68Ga-labelled proteins rapidly under mild conditions in high yields at exceptionally high specific activity and low concentration.
- Berry, David J.,Ma, Yongmin,Ballinger, James R.,Tavare, Richard,Koers, Alexander,Sunassee, Kavitha,Zhou, Tao,Nawaz, Saima,Mullen, Gregory E. D.,Hider, Robert C.,Blower, Philip J.
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p. 7068 - 7070
(2011/08/22)
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- Efficient synthetic access to cationic dendrons and their application for ZnO nanoparticles surface functionalization: New building blocks for dye-sensitized solar cells
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A new concept for the efficient synthesis of cationic dendrons, 4-tert-butyl-1-(3-(3,4-dihydroxybenzamido)benzyl)pyridinium bromide (17), 1,1′-(5-(3,4-dihydroxybenzamido)-1,3-phenylene)bis(methylene) bis(4-tert-butylpyridinium) bromide (18), N1,N7-bis(3-(
- Gnichwitz, Jan-Frederik,Marczak, Renata,Werner, Fabian,Lang, Nina,Jux, Norbert,Guldi, Dirk M.,Peukert, Wolfgang,Hirsch, Andreas
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p. 17910 - 17920
(2011/03/16)
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- DENDRITIC MOLECULAR INTRACELLULAR TRANSPORTERS AND METHODS OF MAKING AND USING SAME
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In accordance with the purpose(s) of the invention, as embodied and broadly described herein, the invention, in one aspect, relates to compounds comprising the structure: and at least one guanidinium residue, wherein m is zero or a positive integer. Also disclosed are methods of preparing the disclosed compounds. Also disclosed are methods of intracellular delivery comprising administering the disclosed compounds and compositions to a subject. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of one or more compounds or compositions of the invention and a pharmaceutically acceptable carrier. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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Page/Page column 84
(2010/11/30)
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- Synthesis, Langmuir and Langmuir-Blodgett film behaviour of new dendritic amphiphiles
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New amphiphilic compounds 1-9 that feature a construction with dendronized hydrophilic and hydrophobic segment groups connected to a specific aromatic or aliphatic spacer unit have been synthesized, following a modular building block strategy. The hydroph
- Akpo, Claudia,Weber, Edwin,Reiche, Juergen
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p. 1820 - 1833
(2008/02/05)
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- SUGAR CHAIN LIGAND COMPOSITE AND METHOD OF ANALYZING PROTEIN WITH THE LIGAND COMPOSITE
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A novel ligand conjugate which is effectively utilizable for analyzing a function of a protein; a ligand-supporting object; and a method of analyzing a protein. The ligand conjugate has a structure which comprises: a linker compound having a structure represented by the following General Formula (1): (wherein n and p each is an integer of 0 to 6) in which X is a structure comprising one, two, or three hydrocarbon derivative chains which have an aromatic amino group at the end and may have a carbon-nitrogen bond in the main chain, Y is a hydro-carbon structure containing one or more sulfur atoms, and Z is a straight-chain structure comprising a carbon-carbon bond or carbon-oxygen bond; and a sugar which has a reducing end and is bonded to the linker compound through the aromatic amino group.
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Page/Page column 18
(2010/11/24)
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- LINKER COMPOUND, LIGAND COMPLEX AND PROCESS FOR PRODUCING THEM
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The present invention provides a novel linker compound which minimizes any nonspecific hydrophobic interactions and is capable of easily adjusting the length to a disulfide group subjected to metal bond to thereby enable effective formation of a metal-sulfur bond; novel ligand conjugate and ligand carrier, and a process for producing them. The linker compound is of a structure represented by the following general formula (1) where a, b, d, e are independently an integer of 0 to 6. X has a structure serving as a multi-branched structure moiety including three or more hydrocarbon derivative chains, wherein the hydrocarbon derivative chains each include an aromatic amino group at an end thereof, and may or may not include a carbon-nitrogen bond in a main chain thereof. The ligand conjugate includes the linker compound having a sugar molecule introduced therein.
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Page/Page column 24-25; 26-27
(2010/11/25)
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- T-BUTYL CASCADE POLYMERS
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A method for forming cascade polymers specifically utilizing the amine monomer of the formula The monomer is made by initially reacting nitromethane and CH2═CHCO2-TBu by nucleophilic addition to form the triester nitrotrialkanoate of the formula and then reducing the nitrosubstituent to afford the said amine monomer.
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