[1-Aryl-isochromanes with fluoxetine-like structure].
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Biomedical subjects
Publications and source records attributed to B Unterhalt.
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Oxetacaine (1), known as Tepilta, may be biotransformed to 2-5. After having tried to separate 1-5 by GC we succeeded in finding the HPLC method on Silicagel Si 60 with the eluent MeOH/TBME/HClO4.
The structure of fluoxetin (1) led to the substituted 3'-phenyl-1'-isochromanyl-2-ethylamines 4-9. These are synthesized by ring closure of the 1,2-diphenylethanols 2a-c with 3-chloropropanal-diethylacetal/BF3-etherate and reaction of the chlorides 3a-c with amines. The affinities to the 5-HT2A-receptor and the serotonin transporter are tested.
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The normal titanium levels in the blood of males between 24 and 66 years of age were found to be 11.2 micrograms/l (rsd 4.1). After oral administration of titanium dioxide containing capsules or as powder (anatas) it could be observed that the material can be absorbed from the gastro-intestinal tract. If two titanium dioxide qualities, having different mean particle sizes (0.16 micron and 0.38 micron), are administered orally, the latter shows less absorption, most likely due to agglomeration phenomena. The blood concentration/time correlation shows the type of curves which are characteristic for a persorption mechanism of absorption and reveal a high individual fluctuation. An increase of the administered dose by twice the amount shows only a tendentious response in the corresponding blood levels. The method of analysis was ICP-AES. A pretreatment of the samples in order to eliminate the organic matrix is necessary.
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For the resolution of racemic 2 MBF-Lactol (3) was used. After 40 h an excess of 3 gave a new product, the "modified" MBF-Lactol 6. This has a high enantiomeric selectivity and leads to well crystallized derivatives.
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Mono- and bicyclic isothiazol-3(2 H)-one 1,1-dioxides and tetrahydrosaccharines 7 were produced by oxidation of the 3-unsubstituted isothiazoles 6. Determination of cross reactivity indicates high values for Compounds 7e and 7l.
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Isochroman is substituted and bound to 6-aminopenicillanic acid either directly or by a spacer in 1-position. In addition to the isochromans two homoisochromans are tested. The activities of the new penicillins against grampositive and gramnegative bacteria are compared with those of benzylpenicillin.
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