The metabolism of [14C]eicosa-11,14-dienoic acid was investigated in rat testes in vivo and in vitro. Intratesticular injection of [1-14C]eicosa-11,14-dienoic acid resulted in the appearance of radioactivity (4–30% of 14C in total fatty acids) in 20-carbon trienoic fatty acids and a small amoun...
1.1. When either radioactive eicosa-11,14-dienoic acid or eicosa-11-enoic acid was incubated with rat liver microsomes or fed to rats which were maintained on a fat-deficient diet, the products of desaturation were respectively eicosa-5,11,14-trienoic acid and eicosa-5, 11-dienoic acid rather th...
Brain metabotropic glutamate receptor 2 (mGluR2) has been proposed as a therapeutic target for the treatment of schizophrenia-like symptoms arising from increased glutamate transmission in the forebrain. However, there does not exist a reliable tool for the study of mGluR2 in human neuroimaging....
The goal of this study is to develop a novel brain receptor imaging agent. This study reports the synthesis, characterization and the biological evaluation of 1-((2-methoxyphenyl) piperazine)ferrocenecarboxamide labeled with technetium-99 m (99mTc-MP). The 99mTc-MP was obtained quickly (radiolab...
The cytotoxicity of the anti-leukaemia drug amsacrine (m-AMSA) has been suggested to result from its oxidative metabolism to the corresponding quinonediimine, N1′-methanesulphonyl-N4′-(9-acridinyl)-3′-methoxy-2′, 5′-cyclohexadiene- 1′.4′-diimine (mAQDI). The metabolic fate of mAQDI was ex...
The conclusion that treating cells with 4′-[(9-acridinyl)-amino]methanesulphon-m-anisidide (m AMSA) causes an alkali-dependent decrease in the size of their DNA was reinvestigated. Evidence is presented that alkali is not needed to detect an effect of mAMSA on the sedimentation rate of DNA rele...
A fluorescent SH reagent, N-(9-acridiny1)maleimide (NAM), was used as a fluorescent probe to detect changes in the conformation of phytochrome from pea (Pisum sativum) seedlings during photoconversion between the red-light absorbing form (Pr) and the far-red-light absorbing form (Pfr). NAM-Cys c...
Phase-transfer-catalyzed esterification of various carboxylic acids has been carried out on a microanalytical scale with a new reagent, N-(9-acridinyl)-bromoacetamide, in aqueous/organic two-phase systems. The procedure gives esters showing very high fluorescence intensity in acid solution. The ...
When cultures of PY815 mouse mastocytoma cells were treated with the antitumour agent 4′-[(9-acridinyl)-amino]methanesulphon-m-anisidine (m-AMSA) for 15 min or 2 hr at 37°C then applied to alkaline sucrose density gradients the DNA released was smaller than the DNA of untreated cells. Under si...
In our search for new DNA intercalating ligands, a novel bifunctional intercalator 11-(9-acridinyl)dipyrido[3,2-a:2′,3′-c]phenazine, acdppz (has two potentially effective intercalators via dipyridophenazine(dppz) and acridine which are linked together via C–C bond) and its corresponding Ru(II...
The structure elucidation of 2-butylamino-1,3-thiazino-[4,5,6-kl]acridine, isolated after the reaction of 9-isothiocyanato-acridine with butylamine, is described. The same compound was found to be formed by photochemical cyclization of N-butyl-N'-(9-acridinyl)thiourea. The intense fluoresce...
The syntheses of 2‐(9‐acridinyl)ethyl‐N‐substituted carbamates and their hydrochlorides and 10‐N‐oxides are reported along with biological results in the areas of antineoplastic, antimalarial, and CNS activity screening. The compounds showed negative biological activity in the areas tested.
Inorganic phosphate is essential for all life forms, yet microbes in marine environments are in near constant deprivation of this important nutrient. Organophosphonic acids can serve as an alternative source of inorganic phosphate if microbes possess the appropriate biochemical pathways that all...
SummaryFollowing a previous microbial inoculation, plants can induce broad-spectrum immunity to pathogen infection, a phenomenon known as systemic acquired resistance (SAR). SAR establishment in Arabidopsis thaliana is regulated by the Lys catabolite pipecolic acid (Pip) and flavin-dependent-mon...
A green Passerini three-component reaction of 2-(4-oxo-4,5,6,7-tetrahydro-1H-indol-1-yl)acetic acid with alkyl or aryl isocyanides and aldehydes was reported under aqueous conditions at 35 °C for 1 h, and 21 indolone-N-amino acid derivatives were prepared in high yields of 42%–99%. Their struc...
The impurity profile of amino acids depends strongly on the production process. Since there are many different production methods (e.g. fermentation, protein hydrolysis or chemical synthesis) universal, state of the art methods are required to determine the impurity profile of amino acids produc...
We report on a novel synthesis towards benzofuran-2-yl-methanamine and indol-2-yl-methanamine derivatives by using ortho-methoxy and ortho-nitro substituted phenylacetic acids as starting material, respectively. For each compound series, a key intermediate bearing the oxazole-4-carboxylic acid m...
1.1. A putative agonist for the strychnine-sensitive glycine receptor picolinic acid was tested for its anticonvulsant activities in mice and muscle-relaxant activities in rats and compared with indole-2-carboxylic acid (I2CA), an antagonist for the strychnine-insensitive glycine receptor. Their...
The crystal structure of N-(1-hexadecyl)-d-gluconamide [a = 4.8072(6) Å, b = 46.771(5) Å, c = 5.2885(7) Å, β = 94.37(1)°; monoclinic P21, Z = 2] displays the same molecular conformation and the same monolayer packing-arrangement as its lower homologues described previously. This is at seemi...
The N-dodecyl gluconamide surfactant (C12GA) was synthesized and characterized by infrared and 1H NMR spectroscopy. The solubility, surface activity and rheology in aqueous solution of mixed C12GA and borax were investigated by surface tension measurements, transmission electron microscopy and r...
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