Reserpin, der sedative Wirkstoff ausRauwolfia serpentina Benth
TL;DR: The sedative principle of Rauwolfia serpentina Benth has been isolated in pure crystalline form and its chemistry and pharmacology has been studied as discussed by the authors, and its properties and properties have been investigated.
Abstract: The sedative principle ofRauwolfia serpentina Benth. has been isolated in pure crystalline form and its chemistry and pharmacology has been studied.
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TL;DR: This review covers the literature on simple indole alkaloid and those with a nonrearranged monoterpenoid unit and newly isolated alkaloids, structure determinations, total syntheses and biological activities.
531 citations
TL;DR: This paper shows by example some total syntheses which draw from strategy-enabling advances in methodology and shows how these capabilities can be used to discover and develop new agents of potential pharmaceutical value without recourse to the natural product itself.
Abstract: Natural products have been a rich source of agents of value in medicine. They have also inspired, at various levels, the fashioning of nonnatural agents of pharmaceutical import. Hitherto, these nonnatural derivatives have been primarily synthesized by manipulating the natural product. As a consequence of major innovations in the subscience of synthetic methodology, the capacity of synthesis to deal with molecules of considerable complexity has increased dramatically. In this paper, we show by example some total syntheses which draw from strategy-enabling advances in methodology. Moreover, we show how these capabilities can be used to discover and develop new agents of potential pharmaceutical value without recourse to the natural product itself.
322 citations
01 Jan 1966
TL;DR: The aim of the present Chapter is to review and discuss the pertinent literature dealing with fundamental problems of Rauwolfia alkaloids and benzoquinolizines rather than to review in detail the enormous literature on the pharmacology of these agents.
Abstract: In 1955 Shore, Brodie and coworkers (Shore, Silver and Brodie 1955, Pletscher, Shore and Brodie 1955) discovered that reserpine caused a marked decrease in the concentration of 5-hydroxytryptamine (5-HT) in tissues and a concomitant rise in the urinary excretion of the 5-HT metabolite 5-hydroxyindoleacetic acid. The deep physiological significance of this discovery became even more evident when reserpine soon afterwards was found to affect tissue catecholamines in a similar manner, an effect leading to block of adrenergic transmission mechanisms (Carlsson and Hillarp 1956a, Bertler, Carlsson and Rosengren 1956). Since then numerous papers have appeared, in which the effects of Rauwolfia alkaloids and a group of similarly acting benzoquinolizines (Pletscher, Besendorf and Bachtold 1958) have been further analyzed. Particular interest has been focussed on the mechanism of action on the abovementioned amines and on the relationship between this action and the various pharmacological effects of Rauwolfia alkaloids and benzoquinolizines. It is the aim of the present Chapter to review and discuss the pertinent literature dealing with these fundamental problems rather than to review in detail the enormous literature on the pharmacology of these agents.
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TL;DR: The Darstellung des Alkaloids Serpentin aus den Wurzeln von Rauwolfia serpentina Benth wurde neu ausgearbeitet, und es wurden nach dem neuen Verfahren grossere Mengen Serpentin dargestellt.
Abstract: Die Darstellung des Alkaloids Serpentin aus den Wurzeln von Rauwolfia serpentina Benth. wurde neu ausgearbeitet, und es wurden nach dem neuen Verfahren grossere Mengen Serpentin dargestellt. Die Base wurde durch Salze charakterisiert und die Summenformel neu zu C21H22O3N2 bestimmt. Durch Selendehydrierung, Verseifung und Vergleich des UV.-Spektrums mit bekannten Spektren wurde die Konstitution des Serpentins teilweise abgeklart.
36 citations
TL;DR: Aus den Wurzeln, bzw. Rinden afrikanischer Rauwolfia-Arten (R. vomitoria und R. obscura) wurde Alstonin isoliert und durch kristallisierte Salze und Derivate charakterisiert.
Abstract: Aus den Wurzeln, bzw. Rinden afrikanischer Rauwolfia-Arten (R. vomitoria und R. obscura) wurde Alstonin isoliert und durch kristallisierte Salze und Derivate charakterisiert.
20 citations
TL;DR: Die funktionellen Gruppen des Indolalkaloids Ajmalin (Rauwolfin) werden aufgeklärt and die Base wird mit Natronkalk and mit Zinkstaub destilliert, die Abbauresultate lassen vermuten.
Abstract: Die funktionellen Gruppen des Indolalkaloids Ajmalin (Rauwolfin) werden aufgeklart und die Base wird mit Natronkalk und mit Zinkstaub destilliert. Die Abbauresultate lassen vermuten, das es sich beim Ajmalin um einen Korper handelt, der Strukturelemente des Strychnins enthalt. Als weniger wahrscheinliche Alternative wird eine Struktur vorgeschlagen, die der Yohimbinformel nahesteht.
18 citations