Two new short-acting non-depolarizing neuromuscular blocking agents

Résumé Le chlorure de 1,1-octaméthylène et le méthylsulfate de 5,5-octaméthylènebis ont chez le chat un effet de blocage neuro-musculaire non dépolarisant, de courte durée. Les comparaisons faites avec des analogues voisins suggèrent que l'activité de ces composés est influencée par le degré d'empêchement stérique autour des atomes d'azote quaternaire. Les composés inhibent les acétylcholinestérases et s'opposent à des degrés divers aux effects muscariniques de l'acétylcholine.     

The comparative enhancement of the depressant action of alcohol by eight representative ataractic and analgesic drugs

Zusammenfassung Eine Methode zur Messung der Potenzierung von Tranquilizern und Analgetika auf Äthanoldepression wird beschrieben. Unbeweglichkeit von Mäusen wird als Kriterium der Depression genommen. Die fünf Tranquilizer, die gebraucht wurden, haben Äthanol in verschiedenen Graden potenziert. Von den drei analgetischen Drogen hat Morphin, nicht aberd-Propoxyphen und Codein, Äthanolnarkose potenziert.

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This study was supported (in part) by a P.H.S. research grant AC-20 from the Division of Accident Prevention, Bureau of State Services, Public Health Service.     

The synthesis of corticosteroids methylated at C21

Zusammenfassung Die Darstellung der beiden epimeren C₂₁-Methylderivate des 9-Fluorprednisolons wird beschrieben. 9-Fluor-21-methyl-1, 4-pregnadien-11, 17, 21B-triol-3, 20-dion-21-azetat ist ein hochwirksames entzündungshemmendes Steroid, vollkommen frei von Nebenwirkungen der Natrium- und Wasserretention des C₂₁-unsubstituierten 9-Fluorprednisolons.     

Tunable gold catalysts for selective hydrocarbon oxidation under mild conditions

Oxidation is an important method for the synthesis of chemical intermediates in the manufacture of high-tonnage commodities, high-value fine chemicals, agrochemicals and pharmaceuticals: but oxidations are often inefficient. The introduction of catalytic systems using oxygen from air is preferred for 'green' processing. Gold catalysis is now showing potential in selective redox processes, particularly for alcohol oxidation and the direct synthesis of hydrogen peroxide. However, a major challenge that persists is the synthesis of an epoxide by the direct electrophilic addition of oxygen to an alkene. Although ethene is epoxidized efficiently using molecular oxygen with silver catalysts in a large-scale industrial process, this is unique because higher alkenes can only be effectively epoxidized using hydrogen peroxide, hydroperoxides or stoichiometric oxygen donors. Here we show that nanocrystalline gold catalysts can provide tunable active catalysts for the oxidation of alkenes using air, with exceptionally high selectivity to partial oxidation products ( approximately 98%) and significant conversions. Our finding significantly extends the discovery by Haruta that nanocrystalline gold can epoxidize alkenes when hydrogen is used to activate the molecular oxygen; in our case, no sacrificial reductant is needed. We anticipate that our finding will initiate attempts to understand more fully the mechanism of oxygen activation at gold surfaces, which might lead to commercial exploitation of the high redox activity of gold nanocrystals.