- Nanofiltration membranes with modified active layer using aromatic polyamide dendrimers
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The modification of a commercial nanofiltration (NF) membrane (TFC-S) with shape-persistent dendritic molecules is reported. Amphiphilic aromatic polyamide dendrimers (G1-G3) are synthesized via a divergent approach and used for membrane active layer modi
- Gao, Yuan,De Jubera, Ana M. Saenz,Marinas, Benito J.,Moore, Jeffrey S.
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- Self-diffusion of hydrophilic poly(propyleneimine) dendrimers in poly(vinyl alcohol) solutions and gels by pulsed field gradient NMR spectroscopy
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Pulsed-field gradient NMR spectroscopy was used to study the diffusion of three different poly(propyleneimine) dendrimers with hydrophilic triethylenoxy methyl ether terminal groups (generations 2, 4, and 5) in poly(vinyl alcohol) aqueous solutions and gels. The effects of the diffusant size, polymer concentration (from 0 to 0.26 g/mL), and temperature on the self-diffusion coefficients have been studied, and the model of Petit et al. [Macromolecules 1996, 29, 6031] was used to fit the experimental data. The Stokes-Einstein hard-sphere radii were also calculated in the zero concentration limit and were compared with those of the linear poly(ethylene glycol)s under the same conditions. The proton NMR relaxation times (T1 and T2) were measured to study the mobility of the dendrimer core part and terminal group as a function of the dendrimer size.
- Bailie,Malveau,Zhu,Kim,Ford
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- Synthesis of Vitamin-B12 Derivatives with Peripheral Tris(oxyethylene) Chains
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The new derivatives 7a-c, of vitamin B12, with a peripheral tris(oxyethylene) chain linked to the corrin ring by an amide or ester group, are prepared, and their ligand-exchange reactions are investigated. Upon reduction of the aqua-cyano complexes 8a-c with NaBH4, cleavage of the 'outer' ester and amide group is observed.
- Pfammatter, Michael J.,Darbre, Tamis,Keese, Reinhart
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- Water-soluble aminocurdlan derivatives by chemoselective azide reduction using NaBH4
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Water-solubility can often enhance the utility of polysaccharide derivatives, for example in pharmaceutical and biomedical applications. Synthesis of water-soluble aminopolysaccharides, particularly those bearing other sensitive functional groups, can be a challenging endeavor. Curdlan is a bioactive β-1,3-glucan with considerable promise for biomedical applications. Aminocurdlans are intriguing target molecules for study of, for example, their interactions with the proteins that form tight junctions between enterocytes. Herein we report the preparation of two water-soluble 6-aminocurdlans starting from 6-bromo-6-deoxycurdlan. The 6-bromide was first displaced by nucleophilic substitution with sodium azide in dimethyl sulfoxide. The O-2 groups were acylated with hydrophilic oligo (ethylene oxide) esters, so as to enhance aqueous solubility. The resultant 6-azido-6-deoxy-2,4-di-O-trioxadecanoylcurdlan was then treated with excess sodium borohydride to reduce the azide; unexpectedly, the water-soluble product proved to be the amide, 6-trioxadecanamido-6-deoxycurdlan. Regioselectivity and degree of substitution (DS) of those derivatives were characterized by means of 1H NMR, 13C NMR and FTIR-spectroscopy, elemental analysis, and titration. Alternatively, direct borohydride reduction of the parent 6-azido-6-deoxycurdlan afforded 6-amino-6-deoxycurdlan that was also water-soluble.
- Zhang, Ruoran,Edgar, Kevin J.
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- NOVEL OPIOID COMPOUNDS AND USES THEREOF
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This invention relates to novel opioid derivatives of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R3, R4 and Z are as defined herein in the disclosure. The invention also relates to the use of such compounds for the treatment or prevention of, for example, pain.
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Paragraph 0480
(2019/09/12)
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- Optically-Detectable Enzyme Substrates and Their Method of Use
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The present invention relates to compounds that are substrates for an enzyme, and upon reaction with the enzyme provide a detectable response, such as an optically detectable response. In particular, the compounds have utility in detecting the presence of a β-lactamase in a sample. In addition to the compounds, methods are disclosed for analyzing a sample for the presence of a β-lactmase, for example, as an indicator of expression of a nucleic acid sequence including a sequence coding for a β-lactmase. Kits are disclosed that include the disclosed compounds and additional components, for example, cells, antibodies, a β-lactmase or instructions for using the components in an assay.
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Paragraph 0400-0401
(2016/06/06)
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- A hydrogen bonding motif for forming extended assemblies
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Oligoamide strands containing tertiary amide groups were found to share a basic structural motif that promotes the formation of H-bonded, chain- or tape-like supramolecular assemblies.
- Zhang, Jiahui,Wu, Xiangxiang,Yamato, Kazuhiro,Liu, Futao,Su, Tianyi,Zheng, Chong,He, Lan,Gong, Bing
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supporting information; experimental part
p. 1062 - 1064
(2010/06/17)
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- Ureidopyrimidinones incorporating a functionalizable p-aminophenyl electron-donating group at C-6
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(Chemical Equation Presented) 2-Ureido-4-[1H]-pyrimidinones have been reported to dimerize via quadruple hydrogen bonding systems with dimerization constants >106 M-1 in CDCl3. The dimerization constant, Kdim, is dependent on the solvent as well as the ring-substituents present, where previously alkyl (e.g., R1 = Me) and aromatic moieties (e.g., R1 = p-NO2C 6H4, R1 = C6H2(OC 13H27)3) have been incorporated at the C-6 position. To assess the influence of alternative, functionalizable, electron-donating groups on the dimerization motif and tautomeric distribution of isomers, the synthesis of compounds possessing aminophenyl functionality at the C-6 position has been achieved. NMR spectroscopy chemical shift analysis revealed that compound 2 (R1 = p-NH2C6H 4, R2 = C6H13) existed as the 2-ureido-4-pyrimidinol dimeric DADA array in DMSO-d6, where a dimerization constant of 46 M-1 was determined. This is the first time that a ureidopyrimidinone quadruple hydrogen bonding DADA array has been observed in pure DMSO, a highly polar solvent. The azo-derivative 5 of compound 2 was prepared which also adopted the pyrimidin-4-ol form in DMSO-d6. Compounds 7, 10 and 11 were then synthesized containing a more hydrophilic PEG unit in the lateral chain and the tautomeric distributions were determined.
- Lafitte, Valerie G. H.,Aliev, Abu E.,Hailes, Helen C.,Bala, Kason,Golding, Peter
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p. 2701 - 2707
(2007/10/03)
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- SUBSTITUTED ACETANILIDES AND BENZAMIDES FOR THE TREATMENT OF ASTHMA AND PULMONARY INFLAMMATION
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Substituted acetanilide or benzamide compositions or formulations for delivery by aerosolization are described. The formulation contains an efficacious amount of acetanilide or benzamide compound able to inhibit inflammation in asthmatic lungs. Compounds of the invention are formulated in 5 ml solution of a quarter normal saline having pH between 5.0 and 7.0. The method for treatment of respiratory tract inflammation by a formulation delivered as an aerosol having mass medium average diameter predominantly between 1 to 5 μ, produced by nebulization or dry powder inhaler.
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Page/Page column 25
(2008/06/13)
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- Prodrugs of etoposide and etoposide analogs
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The present invention provides amphiphilic prodrugs comprising a therapeutic compound conjugated to an PEG-oligomer/polymer and methods for using said prodrugs to enable oral drug delivery and/or delivery of drugs across the blood brain barrier into the c
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Page/Page column 23
(2010/02/06)
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- Hepatic enzymatic synthesis and hydrolysis of CoA esters of solvent-derived oxa acids
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Many ethylene glycol-derived solvents are oxidized to xenobiotic alkoxyacetic acids (3-oxa acids) by hepatic enzymes. The toxicity of these ubiquitous solvents has been associated with their oxa acid metabolites. For many xenobiotic carboxylic acids, the toxicity is associated with the CoA ester of the acid. In this study, related alkoxyacetic acids were evaluated as potential substrates for acyl-CoA synthetases found in mitochondrial, peroxisomal, and microsomal fractions isolated from rat liver. Likewise, chemically synthesized oxa acyl-CoAs were used as substrates for acyl-CoA hydrolases associated with the same rat liver fractions. Activities of the xenobiotic oxygen-substituted substrates were compared with analogous physiologic aliphatic substrates by UV-vis spectrophotometric methods. All of the solvent-derived oxa acids were reasonable substrates for the acyl-CoA synthetases, although their activity was usually less than the corresponding physiologic acid. Acyl-CoA hydrolase activities were decreased compared with acyl-CoA synthetase activities for all substrates, especially for the oxa acyl-CoAs. These studies suggest that these xenobiotic carboxylic acids may be converted to reactive acyl-CoA moieties which will persist in areas of the cell proximal to lipid synthesis, β-oxidation, protein acylation, and amino acid conjugation. The interaction of these xenobiotic acyl-CoAs with those processes may be important to their toxicity and/or detoxification.
- Panuganti, Sree D.,Penn, Jill M.,Moore, Kathleen H.
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- Synthesis of ω-substituted alkanethiols and (bromomethyl)methylthiomalonates
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Several multifunctional derivatives of methylthiomalonic acid (= 2-(thiocarboxy)acetic acid), i.e. 20a,b, 21, 22a,b, and 24, were prepared from thiols bearing a functionalized head group, i.e. from 9a,b, 12, and 16d,f (Schemes 4 and 5). The association constants of the two dithio podands 8b and 11 with K+ were determined.
- Pfammatter, Michael J.,Siljegovic, Vuk,Darbre, Tamis,Keese, Reinhart
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p. 678 - 689
(2007/10/03)
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- Insecticidal substituted-2,4-diaminoquinazolines
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An insecticidal composition comprising, in admixture with an agriculturally acceptable carrier, an insecticidally effective amount of a 2,4-diaminoquinazoline compound of the formula: STR1 wherein R1, R2, R6, R7, W, X, Y, and Z are as defined herein; methods of using the same; novel 2,4-diaminoquinazolines per se; and intermediates in the preparation thereof.
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- Hydrophilic Lipids
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The new triesters of glycerol 1-8 with different oligoethylene glycol carboxylic acids ("hydrophilic lipids") have been synthesized and their complexation with alkali and alkaline earth metal cations has been investigated.
- Heimann, Ulrich,Voegtle, Fritz
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p. 858 - 862
(2007/10/02)
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