Central depressant properties of 3,1-benzoxazine derivatives

Riassunto Sono stati studiati 13 derivati della 3,1-benzossazina, la maggior parte dei quali sono risultati attivi come anticonvulsivanti. Tra di essi il più interessante è risultato il 4H-4-dimetil-6-bromo-3,1-benzossazine-2-one (IV).     

Pharmacological properties of some derivatives of 1,3-benzoxazine

Riassunto Sono stati studiati 22 derivati della 1,3-benzossazina, 8 dei quali sono risultati attivi sulla depressione da reserpina. Tra essi il più efficace è stato il 4H-3-carbossamidometil-1,3-benzossazin-2-one. Correlando la struttura chimica all'attività farmacologica si è visto che la distanza del gruppo amidico dall'anello benzossazinico, la linearità della catena, come pure la presenza di un gruppo amidico libero sono essenziali per l'esplicarsi dell'effetto. Anche sostituzioni in R₄ o nell'anello benzenico portano a perdita dell'attività. Il carbonile in 2 può essere sostituito da un gruppo CS senza sostanziali variazioni di attività.     

Chemical reactivity and biological properties of a series of aminochlorambucil derivatives]

The substitution of aminochlorambucil by a methyl group increased the chemical reactivity in IV b (n = 1) and IV b (n = 2) but their cytotoxicity remained low. The immunosuppressive effect (adjuvant arthritis in Rats and tuberculin related skin reaction) was observed with IV b (n = 2). Aminochlorambucil was effective on adjuvant arthritis only and IV b (n = 1) had no activity. Aminochlorambucil, IV b (n = 1) and IV b (n = 2) were devoid of any non-specific anti-inflammatory activity.     

Serological studies on tomato mosaic virus

Résumé La souche du virus en mosaique de la tomate et celle du virus en mosaique du tabac se sont trouvées alliées comme l'ont montré les résultats des expériences de précipitation et d'aglutination.     

Antiviral properties of 1-allyl and 1-crotyl derivatives of 2-(α-hydroxybenzyl) benzimidazole

Zusammenfassung 1-Allylund 1-Crotyl-2-(oxy-benzyl)-Benzimidazol hemmen die Vermehrung von Poliovirus 1, 2 und 3, sowie diejenige der Coxsackieviren A 9 und A 21 und diejenige des ECHO-Virus 11.     

The estrogenic and deciduogenic properties of some estra-1,3,5(10)triene-3,17β-diol derivatives

Zusammenfassung Die östrogene Aktivität von einigen substituierten Östrodiolderivaten wurde in Rattenvaginalabstrichen und Mäuseuterus-Wachstumversuchen nachgewiesen. Die Einführung von 17-Alkyl-, Alkenyloder Alkinylgruppen in die Östradiolgruppierung hatte einen signifikanten Effekt auf die östrogene Aktivität. Das 17-(2-Butinyl)-Derivat von Östradiol war eine der wirksamsten Substanzen in den Östrogen- und Deciduomaversuchen.     

Serological identification of an antigen associated with acute lymphoid leukemia]

Using as references a lymphoblastoid cell line established from the pleural effusion of a lymphosarcoma patient and the corresponding autochtonous reactive serum, absorption typing assays resulted in the identification of a cell surface antigen associated with acute lymphoid leukaemia. This antigen, provisionally termed PON, may also be demonstrated on the cells of some acute myelomonocytic leukaemias and lymphosarcomas.     

Fluorescence of indole derivatives

Zusammenfassung Die Verwendung von 1N Natronlauge und Essigsäureanhydrid bei der Bestimmung von Indolderivaten mit Hilfe der Fluoreszenzmethode erlaubt eine gute Differenzierung zwischen 5-Methoxyindolderivaten (z.B. Melatonin) und anderen Indolen. Versuche zur Verwendung der neuen Methode in biologischem Material, z.B. Epiphysenschnitten, sind im Gange.     

Serological relationships of frogs (Ranidae) and toads (Bufonidae)

Zusammenfassung Das Ergebnis der immunoelektrophoretischen Untersuchungen zeigt einen gewaltigen Unterschied in den serologischen Mustern der Frösche (Ranidae) und Kröten (Bufonidae). Die amerikanischen Vertreter der Ranidae und der Bufonidae haben sehr wenig gemeinsame Serumantigene. Der Mangel an gemeinsamen antigenischen Bestandteilen in ihren Serumproteinen weist sowohl auf eine frühe Evolutionstrennung des Frosches und der Kröte wie auch auf ein merkliches genetisches Auseinandergehen der zwei Stämme während der langen Zeitspanne isolierter Existenz hin.

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The work was supported by grant No. GM-11782 from the U.S. Public Health Service.     

Indoxyl derivatives of drug metabolites

Summary Indoxyl derivatives were detected as minor products among the urinary metabolites of two trial drugs, a benzodiazepine (GP 55 129) and a benzophenone (CGP 11 952). Their structures were elucidated by NMR and mass spectroscopy. Presumably, metabolites containing potential aldehyde functions react spontaneously with endogenous indoxyl. Such derivatives have not hitherto been encountered in drug metabolism.     

Indoxyl derivatives of drug metabolites

Indoxyl derivatives were detected as minor products among the urinary metabolites of two trial drugs, a benzodiazepine (GP 55 129) and a benzophenone (CGP 11 952). Their structures were elucidated by NMR and mass spectroscopy. Presumably, metabolites containing potential aldehyde functions react spontaneously with endogenous indoxyl. Such derivatives have not hitherto been encountered in drug metabolism.