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Showing 1-30 of 32 results for "50070" within Papers
Carolina García-Martínez et al.
The journal of pain : official journal of the American Pain Society, 7(10), 735-746 (2006-10-05)
Vanilloid receptor subunit 1 (TRPV1) is an integrator of physical and chemical stimuli in the peripheral nervous system. This receptor plays a key role in the pathophysiology of inflammatory pain. Thus, the identification of receptor antagonists with analgesic and anti-inflammatory
Catalina Stan et al.
Revista medico-chirurgicala a Societatii de Medici si Naturalisti din Iasi, 110(4), 1027-1030 (2007-04-19)
It is well known that niflumic acid glycinamide has a good antiinflammatory action useful in gum inflammatory diseases. The objective of this study was to obtain new glycinamides of acetylsalicylic acid and indomethacin, which could have a better antiinflammatory action
Lihu Yang et al.
Bioorganic & medicinal chemistry letters, 16(14), 3735-3739 (2006-05-16)
Systematic modification of a screening lead yielded a class of potent glycinamide based CCR2 antagonists. The best compound (55, (2S)-N-[3,5-bis(trifluoromethyl)benzyl]-2-{[2-(1-piperidinyl)ethyl]amino}-2-(3-thienyl)acetamide) displayed good binding affinity (IC50=30 and 39 nM) toward human monocytes and CHO cell expressing human CCR2b, respectively. Functionally, it
Eric Loeser et al.
Analytical chemistry, 79(14), 5382-5391 (2007-05-29)
When mobile-phase salt content is increased, cationic analytes often show increased retention. This effect is generally attributed to chaotropic or ion pairing effects. However, a cation exclusion mechanism could explain the same effects. In this study, experimental conditions were manipulated
Xiaodong Jia et al.
The Journal of organic chemistry, 78(18), 9450-9456 (2013-08-21)
A catalytic α-sp(3) C-H oxidation of peptides and glycine amides was achieved under radical cation salt catalysis in the presence of O2, producing a series of substituted quinolines. The scope of this reaction shows good functional group tolerance and high
C Beyer et al.
Life sciences, 92(10), 576-581 (2013-02-02)
The effect of i.p. injection or oral ingestion of glycinamide, a glycine pro-drug, on two tests for nociception was assessed in ovariectomized Sprague Dawley rats. To explore the potential analgesic effect of glycinamide the vocalization threshold to tail shock (VT)
Samir Abdurahman et al.
Retrovirology, 6, 34-34 (2009-04-10)
Formation of an HIV-1 particle with a conical core structure is a prerequisite for the subsequent infectivity of the virus particle. We have previously described that glycineamide (G-NH2) when added to the culture medium of infected cells induces non-infectious HIV-1
Gottfried K Schroeder et al.
Biochemistry, 46(13), 4037-4044 (2007-03-14)
As a model for mechanistic comparison with peptidyl transfer within the ribosome, the reaction of aqueous glycinamide with N-formylphenylalanine trifluoroethyl ester (fPhe-TFE) represents an improvement over earlier model reactions involving Tris. The acidity of trifluoroethanol (pKa 12.4) resembles that of
Klaus Urbahns et al.
Bioorganic & medicinal chemistry letters, 20(11), 3376-3379 (2010-05-11)
The design, synthesis and pharmacological properties of a novel class of PPARalpha agonists is described. Compound 2 is a novel, potent and specific glycine amide with oral bioavailability in rodents. The compound is active in vivo and alters plasma lipids
Brett C Bookser et al.
Journal of medicinal chemistry, 48(24), 7808-7820 (2005-11-24)
4-(Phenylamino)-5-phenyl-7-(5-deoxy-beta-D-ribofuranosyl)pyrrolo[2,3-d]pyrimidine 1 and related compounds known as "diaryltubercidin" analogues are potent inhibitors of adenosine kinase (AK) and are orally active in animal models of pain such as the rat formalin paw model (GP3269 ED50= 6.4 mg/kg). However, the utility of
Robert J Cherney et al.
Bioorganic & medicinal chemistry letters, 20(8), 2425-2430 (2010-03-30)
We describe the design, synthesis, and evaluation, of gamma-lactams as glycinamide replacements within a series of di- and trisubstituted cyclohexane CCR2 antagonists. The lactam-containing trisubstituted cyclohexanes proved to be more potent than the disubstituted analogs, as trisubstituted analog, lactam 13
Samir Abdurahman et al.
Antimicrobial agents and chemotherapy, 52(10), 3737-3744 (2008-07-23)
Upon maturation of the human immunodeficiency virus type 1 (HIV-1) virion, proteolytic cleavage of the Gag precursor protein by the viral protease is followed by morphological changes of the capsid protein p24, which will ultimately transform the virus core from
Soojin Kwon et al.
Journal of the American Chemical Society, 127(48), 16796-16797 (2005-12-01)
An enantioselective synthesis of the natural antiproliferative agent quinocarcin was achieved by the directed condensation of optically active alpha-amino aldehyde intermediates. Condensation of the N-protected alpha-amino aldehyde 1, prepared in eight steps (19% yield) from (R,R)-pseudoephedrine glycinamide, with the C-protected
Yong Sun et al.
The journal of physical chemistry. B, 109(12), 5919-5926 (2006-07-21)
For the purpose of investigating the tautomerism from glycinamide (G) to glycinamidic acid (G*) induced by proton transfer, we carried out a study of structural interconversion of the two tautomers and the relative stabilizing influences of water during the tautomerization
Lingyun Wu et al.
Bioorganic & medicinal chemistry letters, 21(18), 5573-5576 (2011-07-26)
Subtype specific ligands are needed to evaluate the therapeutic potential of modulating the brain's neuropeptide Y system. The benzothiazepine glycinamide 1a was identified as an NPY5 antagonist lead. While having acceptable solubility, the compound was found to suffer from high
Irene M Lagoja et al.
Chemistry & biodiversity, 1(1), 106-111 (2006-12-29)
Because of their easy availability and their relative chemical stability, urea, formic acid, and glycine might have played a role in the assembly process of nucleobases. In this paper, a short reaction path is described to prepare hypoxanthine starting from
Wei-Qun Jiang et al.
Journal of peptide science : an official publication of the European Peptide Society, 11(10), 627-632 (2005-07-01)
Accurate kinetic measurements of the rate constants for the acidolysis of five N-acetyl-N-(4-methoxybenzyl)-alpha,alpha-trialkyl glycine cyclohexyl amides in TFA were performed at 25 degrees C and the reactions monitored by HPLC. In all cases the results were consistent with a first
Preparation of Imidazolidin-4-ones and Their Evaluation as Hydrolytically Cleavable Precursors for the Slow Release of Bioactive Volatile Carbonyl Derivatives.
Trachsel A, et al.
European Journal of Organic Chemistry, 2012(14), 2837-2854 (2012)
Len Ito et al.
FEBS letters, 585(3), 555-560 (2011-01-18)
Glycine amide (GlyAd), a typically amidated amino acid, is a versatile additive that suppresses protein aggregation during refolding, heat treatment, and crystallization. In spite of its effectiveness, the exact mechanism by which GlyAd suppresses protein aggregation remains to be elucidated.
Stefan Glatzel et al.
Chemical communications (Cambridge, England), 46(25), 4517-4519 (2010-05-21)
Homopolymers of N-acryloyl glycinamide were prepared by reversible addition-fragmentation chain transfer polymerization in water. The formed macromolecules exhibit strong polymer-polymer interactions in aqueous milieu and therefore form thermoreversible physical hydrogels in pure water, physiological buffer or cell medium.
Irene M Lagoja et al.
Chemistry & biodiversity, 2(7), 923-927 (2006-12-29)
A possible reaction mechanism for the dehydration of glycinamide (3) and N,N'-diformylurea (4) yielding hypoxanthine (2) has been investigated. Furthermore, a potential prebiotic route converting hypoxanthine (2) into adenine (1) via phosphate activation followed by substitution reaction with NH3 was
Irene M Lagoja et al.
Chemistry & biodiversity, 4(4), 818-822 (2007-04-20)
Because of their potential prebiotic origin and relative chemical stability, urea, biuret, formic acid, and glycine amide might have played a role in the assembly process of purine bases. In this paper, we describe a short reaction path to purine
Richard Blunt et al.
Bioorganic & medicinal chemistry letters, 21(20), 6176-6179 (2011-09-06)
A screening hit was used as the basis for the core structure of a new series of acylglycinamide GlyT-1 inhibitors. Investigation of the SAR around four areas of diversity used facile chemistry to prepare compounds quickly. By focussing on reducing
Controlled gelation and sintering of monolithic gels prepared from g-alumina fume powder.
Tsai DS and Hsieh CC.
Journal of the American Ceramic Society. American Ceramic Society, 74(4), 830-836 (1991)
Hong Zhao et al.
Bioconjugate chemistry, 17(2), 341-351 (2006-03-16)
The utility of PEGylation for improving therapeutic protein pharmacology would be substantially expanded if the authentic protein drugs could be regenerated in vivo. Diminution of kinetic constants of both enzymes and protein ligands are commonly encountered following permanent bioconjugation with
Synthesis and Characterization of New Bis-Cyclometalated Rhodium and Iridium Complexes Containing the Glycinamidato Ligand.
Graf M, et al.
Zeitschrift fur Anorganische und Allgemeine Chemie, 639(7), 1117-1121 (2013)
Bei Han et al.
Yao xue xue bao = Acta pharmaceutica Sinica, 45(11), 1379-1384 (2011-03-03)
To research the structure-activity relationship (SAR) of glycinamide-bearing compounds that used as inhibitors of dipeptidyl peptidase IV (DPP-IV), P32/98 and compound A were chosen as the leading compounds, heterocycles containing nitrogen atom were introduced to form amide, and different residues
Kurt L Hoffman et al.
Behavioural brain research, 271, 203-211 (2014-06-17)
Studies in humans indicate that acute administration of sub-anesthetic doses of ketamine, an NMDA receptor antagonist, provokes schizophrenic-like symptoms in healthy volunteers, and exacerbates existing symptoms in individuals with schizophrenia. These and other findings suggest that NMDA receptor hypofunction might
Nicolette M Fernandes et al.
The Journal of organic chemistry, 73(16), 6413-6416 (2008-07-11)
Building upon the discovery of Suggs and Pires that N-(2-hydroxyethyl)glycine amides undergo rapid amide cleavage under mild conditions [ Suggs, J. W. ; Pires, R. M. Tetrahedron Lett. 1997, 38, 2227-2230 ], we synthesized the derivatives (4aalpha,8beta,8aalpha)-1-ethylamido-8-hydroxydecahydroquinoline ( 4) and
N.J. Miles et al.
Journal of the Chemical Society. Perkin Transactions 1, 2299-2299 (1985)
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