Their neuropsychotropic activities were investigated using mice and some interaction tests. In the central nervous systems an activity profile similar to that of reserpine was found for the most active compounds 5d and 5e. Compound 5e is mildly antihypertensive in rats.
Die Bindungslangen und Bindungswinkel wurden aus Is) entnommen. Bindungspolarisierbarkeiten stammen von DenbighI6) und Le Fevre"), die lonisierungsenergien teilweise aus I*).versitat des Saarlandes durchgefiihrt.Die Rechnungen wurden auf einem AEG-Telefunken TR 440 des Rechenzentrums der Uni- 5Die Beziehungen zwisehen Struktur und neuropsychotroper Wirkung bei 6 neuen 1,2,3,4-Tetrahydro-8-carbolinen werden untersucht. Die aktivste Verbindung 4b hat ein pharmakologisches Profil, das dem Chlorpromazin ahnelt. Keine der Substanzen hat dopaminerge Eigenschaften. Dopamine Analogous 1,2,3,4-Tetrahydro-fl-carblinesStructure-activity relationships of six new 1,2,3,4-tetrahydro-fl-carhIines were investigated. The most active compound 4b has a profile similar to that of Chloropromazine. None of the compounds exhibit dopaminergic activities. + Auszug aus der Dissertation H. Schulte-Sienbeck, Berlin 1975. a v e r l a g Chemie, GmbH, Weinheim 1978 Doparninanaloge Tetrahydro-0-carboline 13 3 LIAIHI, 1 Abb. 1: Synthese von dopaminanalogen 1,2,3,4-Tetrahydro-~-carboEnen Die im modifizierten Maus-Screen nach und Campbell") sowie einigen Interaktionstesten erhaltenen Ergebnisse sind in Tab. 1 zusammengefafit.The succinimide derivatives la, c and d condense with methyl 2-methoxybenzoate to yield the methoxybenzoylsuccinimides Zb, c and d, which are converted into the chromono[ 2,3-b]pynoline-2-ones 4a, c and d with pyridine hydrochlorid or HBr/acetic acid. Reactions of these compounds are described.
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