Urease inhibition by hydroxamic acids

Summary Ureases from jack beans andRhodototorula pilimanae were observed to be inhibited by primary hydroxamic acids but were not inhibited by acyclic-secondary (N-alkyl) hydroxamic acids.This project was supported by a Lamar University organized research grant.     

Effects of certain hydroxamic acids on virus replication

Résumé L'acide oxamyl-hydroxamique, l'acide salicylhydroxamique et l'acétoxyoxamide inhibent la reproduction du bactériophage T₄ dans l'Escherichia coli B. L'activité de chacun de ces composés était plus grande que celle de l'hydroxyurée dans le même système d'essai. De ce fait, une évaluation plus poussée de ces 3 agents ainsi que d'autres acides hydroxamiques dans une série de systèmes d'essai sur les virus paraît clairement indiquée.     

Antagonism by deoxyribosides of the inhibitory action of certain hydroxamic acids on deoxyribonucleic acid synthesis

Résumé L'action inhibitrice de l'hydroxyurée (HU) sur une synthèse de DNA peut être antagonisée par des déoxyribosides (dR). De même, un mélange de déoxyadénosine, de déoxyguanosine, et de déoxycytidine annule complètement l'action de l'acide oxanyl hydroxamique (OHA) et inverse, en partie, les effets de l'acide salicylhydroxamique (SHA) et de l'acide (dihydroxybenzoyl-2.3)-hydroxamique (DHB). Lorsqu'on ajoute de la thymidine à une solution de dR, le schéma général d'antagonisme est similaire. De plus, en présence des quatre dR, l'action de l'acétoxyoxamide (AOA) est en partie antagonisée. Il a été conclu que ces acides hydroxamiques, comme l'HU, interviennent, à un degré plus ou moins grand, avec réduction des ribosides.

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Aided by grant No. GM-13958 from the National Institutes of Health, United States Public Health Service.     

The generality of the nitroso-glyoxylate reaction: Conversion ofp-nitronitrosobenzene to the hydroxamic acid

Summary The reaction of glyoxylic acid withp-nitronitrosobenzene (1b) in dilute aqueous solution gave the hydroxamic acid (2b) as the major detectable product. The significance of this observation with respect to the title reaction is discussed.This study was supported by grant No. CA 32395 from the National Cancer Institute, and by Research Career Development Award ES 00120 from the National Institute of Environmental Health Sciences, DHHS.     

Synthesis, structure and function of poly-α-amino acids – the simplest of protein models

During the 1950s, linear and multichain poly-α-amino acids were synthesized by polymerization of the corresponding N-carboxyamino acid anhydrides in solution in the presence of suitable catalysts. The resulting homo- and heteropolymers have since been widely employed as simple protein models. Under appropriate conditions, poly-α-amino acids, in the solid state and in solution, were found to acquire conformations of an α-helix and of β-parallel and antiparallel pleated sheets, or to exist as random coils. Their use in experimental and theoretical investigations of helix-coil transitions helped to shed new light on the mechanisms involved in protein denaturation. Conformational fluctuations of peptides in solution were analysed theoretically and studied experimentally by nonradiative energy-transfer techniques. Poly-α-amino acids played an important role in the deciphering of the genetic code. In addition, analysis of the antigenicity of poly-α-amino acids led to the elucidation of the factors determining the antigenicity of proteins and peptides. The synthetic procedures developed made possible the preparation of immobilized enzymes which were shown to be of considerable use as heterogeneous biocatalysts in the chemical and pharmaceutical industry. Interest in the biological and physicochemical characteristics of poly-α-amino acids was recently renewed because of the reported novel findings that some copolymers of amino acids are effective as drugs in multiple sclerosis, and that glutamine repeats and reiteration of other amino acids occur in inherited neurodegenerative diseases.     

Circadian variations of muscle metabolites

Resumen El contenido diafragmático de proteína, glucógeno y DNA fue estudiado a intervalos de 4 h durante las 24 h. Los animales empleados fueron ratones hembras mantenidos en cuartos con períodos de luzoscuridad de 12 h cada uno. Pudo demostrarse que los tres parámetros presentaron una clara variación circadiana, coincidiendo la aparición de los valores máximos y mínimos para todos ellos durante el período de actividad (oscuridad) y reposo (luz) respectivamente.

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The authors carried out this work with the aid of grants from the Consejo Nacional de Investigaciones Científicas y Técnicas and Comisión de Investigaciones Cientificas de la Provincia de Buenos Aires.     

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.     

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.     

Structure and activity of corticotrophic peptides: Synthesis and biological activity of two corticotrophic peptides with neutral amino acids in positions 17 and 18

Zusammenfassung [D-Ser¹, Nva^17,18]--Corticotropin-(1-19)-nonadecapeptidamid Xa und [D-Ser¹, Nle^17,18]--Corticotropin-(1-19)-nonadecapeptidamid Xb wurden synthetisiert und ihre biologischen Aktivitäten diskutiert.     

(−)-Δ8-tetrahydrocannabinol: Two novel in vitro metabolites

Zusammenfassung (–)-⁸-Tetrahydrocannabinol ist einer der Aktivstoffe in Marihuana (Cannabis sativa L.). Inkubation dieser Verbindung mit der überstehenden Zentrifugationsfraktion (9000g) aus männlicher Hundeleber ergab zwei Hauptmetaboliten, welche durch Massenspektrometrie und Kernresonanzspektroskopie identifiziert wurden. Den beiden Verbindungen werden die Strukturen des 1-Hydroxy-⁸-tetrahydrocannabinols und des 3-Hydroxy-⁸-tetrahydrocannabinols zugeordnet.     

Two novel metabolites ofAspergillus fonsecaeus

Resumen DelAspergillus fonsecaeus (N. R. R. L. 67, O 16-1) se han aislado dos nuevos pigmentos que fueron identificados como monometil éteres de la fonsecina y de la rubrofusarina, respectivamente.

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Acknowledgement. The authors thank Prof.S. Shibata of Tokio University for reference compound, the Cátedra de Microbiologia Industrial of their Faculty for fermentation work and the Consejo Nacional de Investigaciones Cientificas y Técnicas for a grant.     

Antimicrobial metabolites of the marine spongeAxinella polycapella

Summary Extracts of the marine spongeAxinella polycapella contain 1,2,4-trihydroxybenzene (1) and 2,2,4,4,5,5-hexahydroxybiphenyl (3) as antimicrobial constituents. Methods of synthesizing3 by, oxidative dimerization of1 were examined.Acknowledgment. We are grateful to Dr Klaus Reutzler for identifying the sponge and one of us (SW) is pleased to acknowledge fellowship support (1-F32-AI_05883-02) from the Public Health Service.     

Urinary metabolites of bromosulfophthaleine in normal rat

Riassunto E'stata eseguita un'indagine mediante una nuova tecnica cromatografica sull'elimmazione urinaria della BSF nel ratto normale in condizioni fisiologiche, dopo somministrazione endovenosa di 5 e 20 mg/kg di colorante. Si è dimostrato che con il variare del dosaggio si hanno modi d'eliminazione completamente diversi in termini temporali e qualitativi.     

Indole metabolites ofPenicillium cyclopium NRRL 6093

Summary The indoles penitrem A and B and roquefortine were isolated from fungal cultures ofPenicillium cyclopium grown on Czapek-Dox medium at 25°C for 2 weeks.Acknowledgment. We thank Ms. C.E. Johnson for microanalyses. The mention of firm names or trade products does not imply that they are endorsed or recommended by the U.S. Department of Agriculture over other firms or similar products not mentioned.