Search results for "DISCOVERY"
showing 10 items of 4119 documents
A new synthesis of soluble poly(1,4-phenylenevinylene)s and poly(2,5-pyrimidinylenevinylene)s
1991
Abstract Alkoxy-substituted 4-methylbenzylideneanilines 2a-f and their pyrimidine analogues 2g,h show an efficient selfcondensation in the alkaline medium KOC(CH 3 ) 3 /DMF. The totally stereoselective reaction yields 3a-h which are transformed by acidic work-up to 4a-h . A narrow distribution of the molecular weight can be achieved.
Chiral synthetic pseudopeptidic derivatives as triplet excited state quenchers
2009
The behavior of 6 pseudopeptidic models, synthesized by connecting different protected amino acids (Trp, Tyr, Phe, and Lys) with various diamino spacers, as quenchers of the triplet excited state of tiaprofenic acid (and its methyl ester), has been investigated. A series of quenching constants have been determined, which depend on the nature of the quencher and on the stereochemistry of the excited drug. A significant degree of stereodifferentiation has been found for the peptidomimetic synthesized with Phe and Tyr linked by a piperazine bridge. The obtained results support the utility of laser flash photolysis (LFP) as a tool to investigate the interactions between photoexcited drugs and s…
‘Interrupted’ diazotization of 3-aminoindoles and 3-aminopyrroles
2014
Abstract ‘Interrupted’ diazotization of 3-aminoindoles and 3-aminopyrroles, achieved by quenching with cold water immediately after the addition of nitrite, led, in good yields, to stable compounds whose structures were identified to be the diazonium species with nitrate as the counter ion, which show no saline character.
Efficient alkali iodide promoted 18F-fluoroethylations with 2-[18F]fluoroethyl tosylate and 1-bromo-2-[18F]fluoroethane
2003
Abstract Radiochemical 18 F-fluorination yields of several compounds using the secondary labelling precursors 2-[ 18 F]fluoroethyl tosylate ([ 18 F]FETos) and 1-bromo-2-[ 18 F]fluoroethane ([ 18 F]BFE) could be considerably enhanced by the addition of an alkali iodide. The radiochemical yield of [ 18 F]fluoroethyl choline for example could be doubled with [ 18 F]BFE and increased from 13% to ≈80% with [ 18 F]FETos. By addition of alkali iodide to the precursor, the 18 F-fluoroethylation yields of established radiopharmaceuticals, especially in the case of automated syntheses, could be significantly increased without major changes of the reaction conditions.
A study on the aminomercuration-nucleophilic demercuration of --1,5-cyclooctadiene; stereoselective synthesis of 2,6-disubstituted-9-aza bicyclo[3.3.…
1992
Abstract The aminomercuration of cis - cis -1,5-Cyclooctadiene with a series of mercury(II) salts followed by nucleophilic displacement of mercury by aromatic amines, water and nitrate ion has been studied. As a result, bicyclic triamines, aminoalcohols and nitrate esters have been obtained respectively in clean processes which occur under total stereoelectronic control by involvement of a tricyclic aziridium ion to afford a single stereoisomer in each case. The influence of the counter ion and the basicity of the amine on the tandem aminomercuration-demercuration is discussed.
Experimental and DFT study of the conversion of ephedrine derivatives into oxazolidinones. Double SN2 mechanism against SN1 mechanism
2010
Sulfonation of the N-Boc derivatives of 1,2-aminoalcohols, such as ephedrine, pseudoephedrine, norephedrine, norpseudoephedrine, thiomicamine, and chloramphenicol yields a mixture of the corresponding oxazolidinones with inversion (erythro derivatives) and/or retention of configuration (threo derivatives)at C5. We suggest a competition between two mechanisms: an intramolecular SN2 process initiated by attack of the carbonyl oxygen of the Boc group to the benzylic carbon and the other one through a double SN2 process. In the erythro derivatives the first mechanism is predominant, while in the threo derivatives both mechanisms have similar energy. This hypothesis is supported by theoretical c…
Molecular hydrogen (H 2 ) as a potential treatment for acute and chronic fatigue
2020
Many diseases as well as acute conditions can lead to fatigue, which can be either temporary or chronic in nature. Acute fatigue develops frequently after physical exercise or after alcohol hangover, whereas microbial infections such as influenza or COVID-19 and chronic diseases like Parkinson's disease or multiple sclerosis are often associated with chronic fatigue. Oxidative stress and a resulting disturbance of mitochondrial function are likely to be common denominators for many forms of fatigue, and antioxidant treatments have been shown to be effective in alleviating the symptoms of fatigue. In this study, we review the role of reactive oxygen and nitrogen species in fatigue and the an…
Experimental and theoretical investigations for the regio and stereoselective transformation of trans 1,2,3-trisubstituted aziridines into trans oxaz…
2003
The regio and stereoselective transformation of trans 1,2,3-trisubstituted aziridines into trans oxazolidin-2-ones takes place in good yield. However, the cis configuration at C2 and C3 in monocyclic aziridines is a limiting factor for this transformation. Ab initio calculations show that while the ring-opening process assisted by iodide is regioselective, the subsequent ring-closure is responsible for the retention of the configuration at the trans oxazolidin-2-ones. The larger energy found for the ring-closure process for the cis aziridines accounts for the non-formation of the cis oxazolidin-2-ones.
Analysis of the metabolic switch induced by the spirulina peptide SP6 in high fat diet ApoE-/-mice model: A direct infusion FT-ICR-MS based approach
2021
Atherosclerosis, dyslipidemia and hypertension are comorbid diseases often found in combination. Among different pharmacological approaches the employment of natural multifunctional peptides is an attractive option as side therapy. Mass spectrometry-based metabolomics provide valuable information on metabolic changes and can be useful to elucidate peptide pharmacodynamics. In this this work we performed a preliminary investigation on the potential effect of a recently characterized Spirulina platensis peptide named SP6 (GIVAGDVTPI) on the modulation of metabolism in a high fat diet ApoE-/- mice atherosclerotic model. A direct infusion Fourier transform ion cyclotron resonance mass spectrome…
New macrolactones from the defensive salivary secretion of soldiers of the african termite Pseudacanthotermes spiniger
1999
The salivary defensive secretion of large soldier termites of the species Pseudacanthotermes spiniger contains two novel macrocyclic lactones [22-keto-hexacosanolide (2) and 2-hydroxy-24-keto-octacosanolide (3)] together with the already known macrolactone hexacosanolide (1). In addition, the secretion contains important amounts of a polysaccharide based mainly upon β-glucopyranose, β-glucosamine and N-acetyl-β-glucosamine in equal amount.