Synthesis and pharmacological properties of [1-N4-dimethyl-asparagine]-angiotensin II

Summary [1-N⁴-Dimethyl-asparagine]-angiotensin II was synthesized by Merrifield's solid-phase procedure. The analogue gave rat blood pressure about 70% relative potency to Hypertensin (Ciba). Rabbit aorta strips gave intrinsic activity _E=1, a PD₂ of 6.92±0.09 and an affinity relative to [Asn¹]-angiotensin II of 6.5%.The editors do not hold themselves responsible for the opinions expressed in the authors' brief reports. — Les auteurs sont seuls responsables des opinions exprimées dans ces brèves communications. — Für die Kurzmitteilungen ist ausschliesslich der Autor verantwortlich. — Per le brevi comunicazioni è responsabile solo l'autore. — . — Solo los autores son responsables de las opiniones expresadas en estas comunicationes breves.Acknowledgment. The authors wish to express their appreciation to Dr Emanuel Escher, School of Medicine, Centre Hospitalier Universitaire, Sherbrooke, Quebec, for his help in providing the biological data and critical comments.     

Synthesis and pharmacological properties of [1-N4-dimethyl-asparagine]-angiotensin II.

[1-N4-Dimethyl-asparagine]-angiotensin II was synthesized by Merrifield's solid-phase procedure. The analogue gave rat blood pressure about 70% relative potency to Hypertension (Ciba). Rabbit aorta strips gave intrinsic activity alpha E = 1, a PD2 of 6.92 +/- 0.09 and an affinity relative to [Asn1]-angiotensin II of 6.5%.     

Synthesis of the anomeric 9-(2-deoxy-1-D-glucosyl)-adenines and their anhydro derivatives

Zusammenfassung Synthesen von 9-(2-Deoxy-1-D-glukosyl)-adenin und 1-(9-Adenyl)-pseudo-D-glukal werden beschrieben. Diese Substanzen wirken bei der Maus erheblich antileukämisch.     

Synthesis and cytokinin activity of the 3-, 7- and 9-methyl derivatives of zeatin

Zusammenfassung Die 3-, 7- und 9-Monomethylderivative des Cytokinins Zeatin wurden hergestellt und ihre Aktivität in der Karottenwurzel nachgewiesen. Die Ergebnisse zeigen, dass die Nukleotidderivative nicht not-wendige Stufen im Wirkungsmechanismus darstellen.     

Synthesis and properties of praziquantel,a novel broad spectrum anthelmintic with excellent activity against Schistosomes and Cestodes

Summary Synthesis and properties of 2-cyclohexylcarbonyl-1,3,4,6,7,11b-hexahydro-2H-pyrazino [2,1-a] isoquinolin-4-one, a novel anthelmintic with excellent activity against all species of Schistosomes pathogenic to man and a wide range of cestodes, will be reported.     

Synthesis,crystallization and properties of acetyl phenylalanyl lysine chloromethyl ketone: A potential inhibitor of serine proteases

Summary A procedure for the synthesis of acetyl phenylalanyl lysine chloromethyl ketone is described. The chloromethyl ketone derivative is a noncompetitive inhibitor of trypsin (K₁=5.9×10^–3 M).Acknowledgments. The authors are grateful to Dr Arthur L. Bacon for his constant support and encouragement. Special thanks are due to Dr William Kray for initiating this research project. We thank Mrs Juliette Barclay, Ms Earlene Spratling and Ms Ollivette Hill for their technical assistance in conducting some of the experiments. This investigation was supported by MBS grant RR8105 from the General Research Support Branch, Division of Research Resources, National Institutes of Health.     

Synthesis and taste properties of anN-(glucose)-saccharin compound

Résumé La saccharine a été fixée par son azote imidique sur le C₆ du glucose, par l'action de la saccharine sodée sur un dérivé protégé dup-toluénesulfonyl-6-O-d-glucose, et élimination des groupes protecteurs pour former un composé hydrosoluble. La saveur amère peut être attribuée à l'élimination du proton imidique de la saccharine.     

Atomism, Poincaré and Planck

Planck's change in attitude to the question of whether atomic hypotheses were scientifically accessible, is discussed. It is argued contra Holton, that Planck's change in attitude to this question did not signal a methodological shift towards realism. The point of doing this is not just to investigate a significant episode in the history of quantum theory, but also to use the episode as a case study in support of a broader historical thesis. This thesis is that there was a widespread late-nineteenth century methodological tradition which motivated the change in status of certain ontological claims — e.g., that atoms exist — from ‘inaccessible to science’ to ‘scientifically acceptable’ even though those claims were not strictly ‘observable’. This methodological tradition is a hybrid of positivist and realist views. Thus, contrary to one popular view, the fin de siécle triumph of atomism is not to be seen as a triumph for a realist view of science Poincare's views are also used as an illustration.     

Inhibition of the fluorescence of acridine, 9-aminoacridine, and 9-amino-6-chloroacridine by human serum albumin]

Study of fluorescence quenching of acridine and some 9 amino acridines upon human serum albumin additions reveals a single protein fixation site. Characteristic values of thermodynamic functions are obtained from experiments at different temperatures.