Search results for "amide"
showing 10 items of 3119 documents
Mandelamide-zinc-catalyzed enantioselective alkyne addition to heteroaromatic aldehydes.
2006
The (S,S)-mandelamide III catalyzes the additions of both aryl- and alkylalkynylzinc reagents to heteroaromatic aldehydes with good yields and enantioselectivities up to 92%. This catalyst is easily prepared in a one-step procedure, and both enantiomers are available. Unlike most other described methods, using this catalyst does not require the addition of Ti(O(i)Pr)4.
Stabilization of anti-leukemic enzyme l-asparaginase by immobilization on polysaccharide levan
2001
Abstract Biologically active fructose polymer levan from Zymomonas mobilis of different molecular mass (75 and 2000 kDa) was covalently coupled to anti-leukemic enzyme Erwinia carotovora l -asparaginase. The method used for the immobilization of the enzyme involved periodate oxidation of the polysaccharide, followed by reductive alkylation. A gentle periodate oxidation of levan (oxidation degree ≤24%) resulted in the highest residual enzyme activity (≥55%). The K m(app.) of glycoconjugates was higher than the K m of native l -asparaginase. The conjugation of l -asparaginase widened the optimum pH range of the enzyme. The electrophoretic mobility in polyacrylamide gel of glycoconjugates obta…
Benzimidazoles as NMDA Glycine-Site Antagonists: Study on the Structural Requirements in 2-Position of the Ligand
2000
A series of different substituted benzimidazole derivatives has been synthesized and evaluated for the ability to displace [3H]MDL-105,519 to rat cortical membranes. Two benzimidazole-2-carboxylic acids 9 b and 9 c, in this substitution pattern not yet described as glycine antagonists, showed IC50 values of 0.89 microM (9 b) and 38.0 microM (9 c). Replacement of the carboxylate function in 2-position by a sulfonic acid moiety appreciably increased solubility, but decreased the affinity giving evidence for the strong need of the carboxylate group within the ligand. Further structure-activity studies using benzimidazole-2-one derivatives with an acetic acid moiety adjacent to a ring nitrogen …
ChemInform Abstract: Benzimidazoles as NMDA Glycine-Site Antagonists: Study on the Structural Requirements in 2-Position of the Ligand.
2010
A series of different substituted benzimidazole derivatives has been synthesized and evaluated for the ability to displace [3H]MDL-105,519 to rat cortical membranes. Two benzimidazole-2-carboxylic acids 9 b and 9 c, in this substitution pattern not yet described as glycine antagonists, showed IC50 values of 0.89 microM (9 b) and 38.0 microM (9 c). Replacement of the carboxylate function in 2-position by a sulfonic acid moiety appreciably increased solubility, but decreased the affinity giving evidence for the strong need of the carboxylate group within the ligand. Further structure-activity studies using benzimidazole-2-one derivatives with an acetic acid moiety adjacent to a ring nitrogen …
Radioactive labeling of defined HPMA-based polymeric structures using [18F]FETos for in vivo imaging by positron emission tomography.
2009
During the last decades polymer-based nanomedicine has turned out to be a promising tool in modern pharmaceutics. The following article describes the synthesis of well-defined random and block copolymers by RAFT polymerization with potential medical application. The polymers have been labeled with the positron-emitting nuclide fluorine-18. The polymeric structures are based on the biocompatible N-(2-hydroxypropyl)-methacrylamide (HPMA). To achieve these structures, functional reactive ester polymers with a molecular weight within the range of 25,000-110,000 g/mol were aminolyzed by 2-hydroxypropylamine and tyramine (3%) to form (18)F-labelable HPMA-polymer precursors. The labeling procedure…
Long-term biodistribution study of HPMA- ran -LMA copolymers in vivo by means of 131 I-labeling
2018
Abstract Background For the evaluation of macromolecular drug delivery systems suitable pre-clinical monitoring of potential nanocarrier systems is needed. In this regard, both short-term as well as long-term in vivo tracking is crucial to understand structure-property relationships of polymer carrier systems and their resulting pharmacokinetic profile. Based on former studies revealing favorable in vivo characteristics for 18 F–labeled random (ran) copolymers consisting of N-(2-hydroxypropyl)methacrylamide (HPMA) and lauryl methacrylate (LMA) – including prolonged plasma half-life as well as enhanced tumor accumulation – the presented work focuses on their long-term investigation in the li…
High performance PA6/CNTs nanohybrid fibers prepared in the melt
2012
Commercial and home-made carbon nanotubes (CNTs) were plasma treated under oxygen atmosphere and then added to polyamide 6 (PA6) in order to prepare fibres by melt spinning. For comparison, pristine nanofillers were used too. The effect of functionalization and of filler characteristics on the morphological, rheological, mechanical and electrical properties of the fibres was studied by TEM and SEM, rheological measurements, tensile and electrical conductivity tests. The results demonstrated that the functionalization led to a better mechanical performance and the morphological analysis confirmed that the adhesion, the dispersion and the alignment of the nanotubes within the polymer matrix w…
Dinuclear bis(terpyridine)ruthenium(II) complexes by amide coupling of ruthenium amino acids: Synthesis and properties
2011
Abstract Two redox-asymmetric amide-bridged bis(terpyridine)ruthenium(II) complexes (3a, 3b) have been prepared by amide coupling of a carboxylic acid functionalized complex with an amine substituted complex and they were fully characterized by spectroscopic analyses. They emit at 692 and 750 nm at room temperature in fluid solution with quantum yields larger than 10−3 and 3MLCT lifetimes of 22 ns. Ru···Ru distances were estimated from DFT models as 17.7 and 13.4 A for 3a and 3b, respectively. Cyclic voltammetry gives two oxidation potentials for the differently substituted ruthenium sites with splittings of 0.10 and 0.23 V for 3a and 3b, respectively. Oxidation of 3b with CeIV ions gives t…
Solid–liquid extraction of ω-amino acids using ditopic receptors
2008
Abstract Five heteroditopic ligands have been prepared to be used in solid–liquid extraction of ω-amino acids into DMSO solutions. The prepared ligands contain crown ethers as cation binding sites and thiourea or amide groups for anion recognition. The aliphatic zone of the 1H NMR spectra suggests that two different species related to the amino acid are present in solution. One of these species is the complexed zwitterionic form and the other seems to be free non-zwitterionic amino acid. The presence of these two species allows extraction efficiencies higher than 100%.
Redox and Photochemistry of Bis(terpyridine)ruthenium(II) Amino Acids and Their Amide Conjugates – from Understanding to Applications
2014
Invited for the cover of this issue is the group of Katja Heinze at the Johannes Gutenberg University of Mainz, Germany. The cover image shows the bis(terpyridine)ruthenium(II) amino acid [Ru(4′-tpy-COOH)(4′-tpy-NH2)]2+ (tpy = 2,2′;6′,2″-terpyridine), illustrating some of its multifaceted optical and redox chemical properties as well as highlighting its potential applications in light-to-energy conversion and energy-to-light conversion schemes.