Synthesis and biodistribution of p-iodophenyl analogues of a naturally occurring imidazole ribonucleoside

A model iodophenyl imidazole ribonucleoside has been synthesized to study biodistribution properties in laboratory animals. The key intermediate 5-amino-1-(2,3,5-tri-O-acetyl-β-D-ribofuranosyl)imidazole-4-[N-(p-iodophenyl)carboxamide] ( 5 ) was synthesized by coupling N-succinimidyl-5-amino-1-(2,3,5-tri-O-acetyl-β-D-ribofuranosyl)imidazole-4-carboxylate ( 4 ) and p-iodoaniline. Deacetylation of the intermediate compound gave 5-amino-1-β-D-ribofuranosylimidazole-4-[N-(p-iodophenyl)]carboxamide ( 6 ). Ring annulation via diazotization of 5 gave 7-(2,3,5-tri-O-acetyl-β-D-ribofuranosyl)imidazo[4,5-d]-v-triazin-[3-N-(p-iodophenyl)]-4-one ( 7 ). Subsequent deacetylation of 7 afforded 7-β-D-ribofuranosylimidazo[4,5-d]-v-triazin-[3-N-(p-iodophenyl)]-4-one ( 8 ). The radiolabeled compounds, [¹²⁵I] 5 and [¹²⁵I] 6 were prepared in a manner similar to the corresponding unlabeled compounds except that p-[¹²⁵I]iodoaniline was used for coupling with 4 . Biodistribution studies of iodine-125-labeled 5 and 6 were performed in female Fischer rats and tumor bearing nude mice. Compound 6 showed uptake in the brain and proliferating tissues such as tumor and bone-marrow.     

The integration of certain products of the multivariableH-function with a general class of polynomials

The authors present six general integral formulas (four definite integrals and two contour inegrals) for theH-function of several complex variables, which was introduced and studied in a series of earlier papers by H. M. Srivastava and R. Panda (cf., e.g., [25] through [29]; see also [14] through [18], [20], [24], [32], [34], [35], [37], and [38]). Each of these integral formulas involves a product of the multivariableH-function and a general class of polynomials with essentially arbitrary coefficients which were considered elsewhere by H. M. Srivastava [21]. By assigning suiatble special values to these coefficients, the main results (contained in Theorems 1, 2 and 3 below) can be reduced to integrals involving the classical orthogonal polynomials including, for example, Hermite, Jacobi [and, of course, Gegenbauer (or ultraspherical), Legendre, and Tchebycheff], and Laguerre polynomials, the Bessel polynomials considered by H. L. Krall and O. Frink [9], and such other classes of generalized hypergeometric polynomials as those studied earlier by F. Brafman [3] and by H. W. Gould and A. T. Hopper [8]. On the other hand, the multivariableH-functions occurring in each of our main results can be reduced, under various special cases, to such simpler functions as the generalized Lauricella hypergeometric functions of several complex variables [due to H. M. Srivastava and M. C. Daoust (cf. [22] and [23])] which indeed include a great many of the useful functions (or the products of several such functions) of hypergeometric type (in one and more variables) as their particular cases (see,e. g., [1], [10] and [39]). Many of the aforementioned applications of our integral formulas (contained in Theorems 1, 2 and 3 below) are considered briefly. Further usefulness of some of these consequences of Theorems 1 and 2 in terms of the classical orthogonal polynomials is illustrated by considering a simple problem involving the orthogonal expansion of the multivariableH-function in series of Jacobi polynomials. It is also shown how these general integrals are related to a number of results scattered in the literature. 0261 0262 V     

Intensities of wagging and rocking bands of water in MnCl2 · 2H2O and CoCl2 · 2H2O

IR relative integrated intensities and half-widths of rocking (R) and wagging (W) bands of water in MnCl₂ · 2H₂O and CoCl₂ · 2H₂O are presented at 300 K and 120 K. Departure of observed intensity into D_W/D_R from those predicted by the fixed dipole model is attributed to anisotropic dynamic changes in dipole during these oscillations. A quantity representing the variation of this anisotropy between W and R oscillations is computed and its origin is discussed. An increase by 20% to 50% in both D_W and D_R on lowering the temperature has also been discussed.     

An iodine-123 generator/iodination kit: A preliminary report

Preliminary results are described of a¹²³Xe filled device to serve as a combination¹²³I generator/iodination kit.¹²³X was produced in the Brookhaven Linac Isotope Producer (BLIP) by the reaction¹²⁷I(p, 5n)¹²³Xe. The device consists of a small glass ampoule containing an internal glass breakseal and a flanged neck on which was crimped a multi-injection type septum. The ampoule contained a hydrogen sulfide atmosphere to assure that the iodine generated from the decay of the xenon was in the form of iodide. Following an adequate period for¹²³Xe to decay (this period can be used for shipment), a needle is forced through the septum breaking the seal and residual gases are pumped off. The¹²³I in the form of iodide can then be rinsed from the ampoule with any desired solvent or reagent added directly to the device to carry out an iodination in an enclosed environment. Preliminary results of both iodine recovery and iodinations have been promising. This research was supported by the US Department of Energy under Contract No. DE-ACO2-76CH0016.     

Use of p-Cresotic acid and its various derivatives for the estimation of thorium and zirconium

Summary p-Cresotic acid and its nitro, bromo, sulfo, acetyl, benzoyl and hydrazine derivatives and 5-methyl salicylic-o-aeetic acid have been used for the estimation of thorium and zirconium. The precipitates obtained have in all cases been ignited and weighed as oxides. These reagents have been found under suitable experimental conditions to effect the separation of Th as well as Zr from cerite earths.     

Copper(II) ion sensor based on electropolymerized undoped conducting polymers

A solid state copper(II) ion sensor is reported based on the application of electropolymerized undoped (neutral) polycarbazole (PCz) and polyindole (PIn) modified electrodes. The new sensor shows high selectivity to Cu²⁺ ions with a detection limit of 10^–5 M. PCz and PIn are formed respectively by the anodic oxidation of 50 mM carbazole and 5 mM indole monomers in dichloromethane containing 0.1 M tetrabutylammonium perchlorate on a platinum electrode using a single compartment cell. Potentiostatic polymerization of both the monomers are carried out at 1.3 V and 1.0 V vs. Ag/AgCl, respectively. Perchlorate ions were electrochemically removed from the polymer films by applying – 0.2 V vs. Ag/AgCl. Polymer-coated electrodes are incubated in 1 M KCl solution for 8 h followed by incubation in distilled water for 2 h before using as a metal ion sensor. The undoped PCz and PIn electrodes were found to be highly selective and sensitive for Cu²⁺ ions with little selectivity for Pb²⁺ and negligible response towards Ag⁺, Hg²⁺, Cu⁺, Ni²⁺, Co²⁺, Fe²⁺, Fe³⁺ or Zn²⁺. Potentiometric responses for Cu²⁺ ions are recorded for both the sensor electrodes together with a double-junction Ag/AgCl reference electrode. Calibration curves for Cu²⁺ are reported for both ion sensors. The polymer-modified electrodes were found to be stable for several weeks. Electronic Publication     

On the estimation of higher order resistance coefficients from electroosmotic transport data

Summary First and second order resistance coefficients between membrane matrix and permeant for the permeation of methanol, acetone and methyl ethyl ketone through pyrex and quartz membranes have been evaluated from the experimental data on electroosmotic effects. Analysis of the data shows that-the following non-linear relationP =R ₁₁ J _v +R ₁₂ I +R ₁₂₂ I ²[1] exists between pressure difference,P, and the fluxes and a linear relation =R ₂₁ J _v +R ₂₂ I [2] expresses the dependence of potential difference,, on the fluxes. The first order cross resistance coefficients have been found to obey theOnsager's reciprocity relation. An attempt has been made to explain the occurrence of higher order resistance coefficients in terms of electrokinetic character of the membrane, permeant interface.

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Zusammenfassung Die Widerstandskoeffizienten 1. und 2. Ordnung zwischen einer Membranmatrix und dem permeierenden Stoff wurden für die Permeation von Methanol, Aceton und Methyläthylketon durch Pyrex- und Quarz-Membranen auf Grund elektroosmotischer Effekte bestimmt. Die Auswertung gibt die nichtlineare BeziehungP =R ₁₁ J _v +R ₁₂ I +R ₁₂₂ I ² [1] zwischen der Druckdifferenz und dem Fließen; die lineare Beziehung =R ₂₁ J _v +R ₂₂ I [2] beschreibt die Abhängigkeit der Potentialdifferenz vom Fließen. Die gekreuzten Widerstandskoeffizienten 1. Ordnung gehorchen dem ReziprozitätsgesetzOnsager. Das Vorkommen von Widerstandskoeffizienten höherer Ordnung wird versuchsweise auf den elektrokinetischen Charakter der Membran-Grenzfläche zurückgeführt.

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With 2 figures and 2 tables     

Mass spectrometric determination of the heats of formation of the silane bromides

The reaction of SiBr₄(g) with H₂(g) in the temperature range 900–1143 K has been studied by a mass spectrometric method. Second and third law reaction enthalpies were obtained for SiBr₄(g) + H₂(g) = SiHBr₃(g) + HBr(g), SiHBr₃(g) + H₂(g) = SiH₂Br₂(g) + HBr(g), and SiH₂Br₂(g) + H₂(g) = SiH₃Br(g) + HBr(g). From the heats of reaction, third-law ΔH_£298 values of ?72.5 ± 1, ?43.2 ± 1.5 and ?15.3 ± 0.5 kcal/mole were obtained for SiHBr₃(g), SiH₂Br₂(g), and SiH₃Br(g), respectively.     

Spectrophotometric Determination of Palladium with Methylthymol Blue

A new, sensitive spectrophotometric method for the determination of palladium(II) with methylthymol blue has been developed. The palladium methylthymol blue complex has an absorption maximum at 530 nm. The colour reaction has a sensitivity of 0.005 µg of palladium/cm² and obeys Beer's Law over the range 0.4 to 3.24 ppm of palladium. The effects of concentration of perchloric acid, reagent, heating, stability of colour and diverse ions have been investigated. The ratio of metal: ligand in the complex is 1:1 and the formation constant was calculated to be 1.18×10⁴.